treatment	standardized_cid	clinical_phase	description	mechanism_of_action	targets	epigenetic_class	epigenetic_class_fine
(5Z)-7-Oxozeanol	9863776	Preclinical	Potent and selective transforming growth factor-β-activated kinase 1 (TAK1) mitogen-activated protein kinase kinase kinase (MAPKKK) inhibitor (IC50= 8nM). Displays > 33-fold and > 62-fold selectivity over MEKK1 and MEKK4 respectively. Inhibits IL-1-induced activation of NF-κB (IC50= 83 nM) and JNK/p38. Inhibits production of inflammatory mediators, and sensitizes cells to TRAIL- and TNF α-induced apoptosis in vitro.	tak1 inhibitor	TAK1	Non-epigenetic	Non-epigenetic
131I-MIBG	71184	N/A	Metaiodobenzylguanidine (MIBG) labeled with the radioactive isotope iodine-131 is a form of radiotherapy used in the treatment of neuroendrocrine tumors and neuroblastomas	radiation therapy	MIBG	Non-epigenetic	Non-epigenetic
131I-MIBG + Irinotecan		N/A | Launched	Combination: 131I-MIBG + Irinotecan	radiation therapy | topoisomerase inhibitor	CYP3A5 | TOP1 | TOP1MT	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
131I-MIBG + Vorinostat		N/A | Launched	Combination: 131I-MIBG + Vorinostat	hdac inhibitor | radiation therapy	HDAC1 | HDAC10 | HDAC11 | HDAC2 | HDAC3 | HDAC5 | HDAC6 | HDAC8 | HDAC9	Eraser | Non-epigenetic	HDACi | Non-epigenetic
3-Fluorobenzylspiperone maleate	24978532	Preclinical	3'-Fluorobenzylspiperone maleate is a very potent and selective ligand for the D2 receptor (Ki = 0.023 nM). Compared with spiperone, displays a 2.5-fold greater affinity at D2 and a 12-fold lower affinity at 5-HT2 receptors	d2 receptor antagonist	D2	Non-epigenetic	Non-epigenetic
4Gy IR		N/A	Low-dose radiation therapy	radiation therapy		Non-epigenetic	Non-epigenetic
5-Fluorouracil	3385	Launched	Analogue of uracil and a potent antitumor agent. 5-Fluorouracil affects pyrimidine synthesis by inhibiting thymidylate synthetase thus depleting intracellular dTTP pools. 5-Fluorouracil induces apoptosis and can be used as a chemical sensitizer	thymidylate synthase inhibitor	CD44 | DPYD | TYMS	Non-epigenetic	Non-epigenetic
9-ing-41		Phase 2	9-ING-41 (Elraglusib) is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic agents.	gsk3b inhibitor	GSK3B | MARK2	Non-epigenetic	Non-epigenetic
A939572	24905400	Preclinical	A939572 is a potent, and orally bioavailable stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50 values of <4 nM and 37 nM for mSCD1 and hSCD1, respectively.	stearoyl-coa desaturase inhibitor	SCD	Non-epigenetic	Non-epigenetic
ABBV-744	132010322	Phase 1	BDII-selective BET bromodomain inhibitor that inhibits BRD2, BRD3 and BRD4.	bromodomain inhibitor	BRD2	Reader	PAHi
Abemaciclib	46220502	Launched	Abemaciclib is an orally available cyclin-dependent kinase (CDK) inhibitor that targets the CDK4 (cyclin D1) and CDK6 (cyclin D3) cell cycle pathway, with potential antineoplastic activity.	cdk inhibitor	CDK4 | CDK6	Non-epigenetic	Non-epigenetic
Abexinostat	11749858	Phase 3	Abexinostat (CRA 024781) is a novel pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM. Abexinostat also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC50 below 10 nM	hdac inhibitor	HDAC1 | HDAC10 | HDAC2 | HDAC3 | HDAC6 | HDAC8	Eraser	HDACi
Abiraterone	132971	Launched	Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.	androgen biosynthesis inhibitor	CYP11B1 | CYP17A1	Non-epigenetic	Non-epigenetic
ABT751	3035714	Phase 2	ABT-751 (E7010) is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer	tubulin polymerization inhibitor	TUBB	Non-epigenetic	Non-epigenetic
ABT888	11960529	Phase 3	Veliparib (ABT-888) is a potent PARP inhibitor, inhibiting PARP1 and PARP2 with Kis of 5.2 and 2.9 nM, respectively	parp inhibitor	PARP1 | PARP2	Non-epigenetic	Non-epigenetic
AC-93253 iodide	16078948	Preclinical	AC-93253 is a selective, potent SIRT2 inhibitor. AC93253 can inhibit SIRT2 with an IC50 value of 6 μM. AC93253 can be used for the research of tumors.	sirt2 inhibitor	SIRT2	Eraser	HDACi
Acalabrutinib	71226662	Launched	Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL). Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups	bruton's tyrosine kinase (btk) inhibitor	BTK	Non-epigenetic	Non-epigenetic
Actinomycin D	457193	Launched	Actinomycin D (Dactinomycin, Act D, RASP-101) is a significant polypeptide antibiotic isolated from soil bacteria of the genus Streptomyces. Actinomycin D (Dactinomycin) inhibits DNA repair and rests the cell cycle at G1 phase with IC50 of 0.42 μM and 0.4 nM, respectively. Actinomycin D is an autophagy activator, induces p53-independent cell death and prolongs survival in high-risk chronic lymphocytic leukemia.	rna polymerase inhibitor	POLR2A	Non-epigenetic	Non-epigenetic
ACY-1035	76281032	Preclinical	Selective inhibitor of HDACs	hdac inhibitor	HDAC1 | HDAC2 | HDAC3	Eraser	HDACi
ACY-1035 + Doxorubicin		Preclinical	Combination: ACY-1035 + Doxorubicin	hdac inhibitor | topoisomerase inhibitor	HDAC1 | HDAC2 | HDAC3 | TOP2	Eraser | Non-epigenetic	HDACi | Non-epigenetic
Adagrasib	138611145	Phase 3	Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction.	ras gtpase inhibitor	KRAS	Non-epigenetic	Non-epigenetic
Adagrasib + Palbociclib		Phase 3 | Launched	Combination: Adagrasib + Palbociclib	cdk inhibitor | kras inhibitor	CCND3 | CDK4 | CDK6 | KRAS	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Adavosertib	24856436	Phase 2	Potent Wee1 inhibitor with an IC50 of 5.2 nM.	wee1 kinase inhibitor	WEE1	Non-epigenetic	Non-epigenetic
ADH1	9916058	Phase 2	ADH-1 trifluoroacetate is an N-cadherin antagonist, which inhibits N-cadherin mediated cell adhesion.	cadherin antagonist	CDH2	Non-epigenetic	Non-epigenetic
AEE788	10297043	Phase 1/Phase 2	AEE788 is an inhibitor of the EGFR and ErbB2 with IC50 values of 2 and 6 nM, respectively	egfr inhibitor | vegfr inhibitor	EGFR | ERBB2 | ERBB4 | FGFR2 | FGFR3 | FLT1 | KDR	Non-epigenetic	Non-epigenetic
Afatinib	10184653	Launched	Irreversibly inhibits EGFR/HER2 including EGFR(wt) ,EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5nM, 0.4nM, 10nM and 14nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant. Phase 3	egfr inhibitor	EGFR | ERBB2 | ERBB4	Non-epigenetic	Non-epigenetic
AICAR	17513	Phase 3	AICAR stimulates mitochondrial metabolism as an AMPK agonist	ampk activator	AMPK	Non-epigenetic	Non-epigenetic
Akt Inhibitor IV	5719375	Preclinical	Akt inhibitor-IV (AKTIV) acts as a PI3K-Akt inhibitor at the E isomer (HY-14971), with potent cytotoxicity	pi3k-akt inhibitor	PI3K-Akt	Non-epigenetic	Non-epigenetic
Albendazole	2082	Launched	Albendazole (SKF-62979) is an orally active and broad-spectrum parasiticide with high effectiveness and low host toxicity, is used for the research of gastrointestinal parasites in humans and animals. Albendazole induces apoptosis and autophagy in cancer cells. Albendazole also inhibits tubulin polymerization and HIF-1α, VEGF expression, has antioxidant activity, and inhibits the glycolytic process in cancer cells	tubulin polymerization inhibitor	CYP1A2 | CYP2J2 | TUBA1A | TUBB | TUBB4B	Non-epigenetic	Non-epigenetic
Alisertib	24771867	Phase 3	Selective Aurora A and Aurora B inhibitor with IC50 values of 1.2 and 396.5 nM, respectively.	aurora kinase inhibitor	AURKA	Non-epigenetic	Non-epigenetic
Alpelisib	56649450	Launched	PI3Kα inhibitor with IC50 of 5 nM, and minimal effect on PI3Kβ/γ/δ. Phase 1/2.	pi3k inhibitor	PIK3CA | PIK3CB | PIK3CD | PIK3CG	Non-epigenetic	Non-epigenetic
Altretamine	2123	Launched	Altretamine is an alkylating antineoplastic agent	dna synthesis inhibitor		Non-epigenetic	Non-epigenetic
Alvocidib	5287969	Phase 2	Alvocidib is the free base form of a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity.	cdk inhibitor	BCL2 | BIRC5 | CCNT1 | CDK1 | CDK2 | CDK4 | CDK5 | CDK6 | CDK7 | CDK8 | CDK9 | EGFR | MCL1 | PYGM | XIAP	Non-epigenetic	Non-epigenetic
AMG208	24864821	Phase 1	AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC50 of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity	tyrosine kinase inhibitor	MET	Non-epigenetic	Non-epigenetic
AMG337	44181686	Phase 2	AMG-337 is a potent, orally active, selective MET kinase inhibitor with IC50 values of 1, 1, 4.7, 5, 21.5, 1077 and >4000 nM of WT MET, H1094R MET, M1250T MET, HGF-stimulated pMET (PC3 cells) MET, V1092I MET, Y1230H MET, and D1228H MET, respectively. AMG 337 inhibits the phosphorylation of MET and downstream effectors in MET-amplified cancer cell lines, resulting in an inhibition of MET-dependent cell proliferation and induction of apoptosis	met inhibitor	MET	Non-epigenetic	Non-epigenetic
AMG900	24856041	Phase 1	AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor with IC50 of 5 nM, 4 nM and 1 nM for Aurora A, B and C, respectivel	aurora kinase inhibitor	AURKA | AURKB | AURKC	Non-epigenetic	Non-epigenetic
Amiloride	16231	Launched	Amiloride (MK-870 HCl) is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).	sodium channel blocker	AOC1 | ASIC1 | ASIC2 | ASIC3 | PKD2 | PKD2L1 | PLAU | SCNN1A | SCNN1B | SCNN1D | SCNN1G | SLC9A1 | TRPC7 | TRPV2	Non-epigenetic	Non-epigenetic
Aminopterin	169371	Phase 3	Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia	dihydrofolate reductase inhibitor	DHFR | SLC46A1	Non-epigenetic	Non-epigenetic
Amonafide	50515	Phase 3	Amonafide is a topoisomerase II inhibitor and DNA intercalator that induces apoptotic signaling by blocking the binding of Topo II to DNA	topoisomerase inhibitor	TOP2A | TOP2B	Non-epigenetic	Non-epigenetic
Amsacrine	2179	Launched	Amsacrine (m-AMSA; acridinyl anisidide) is an inhibitor of topoisomerase II, and acts as an antineoplastic agent which can intercalates into the DNA of tumor cells	topoisomerase inhibitor	KCNH2 | TOP2A	Non-epigenetic	Non-epigenetic
Amuvatinib	11282283	Phase 2	Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity	flt3 inhibitor | kit inhibitor | pdgfr tyrosine kinase receptor inhibitor | rad51 inhibitor | ret tyrosine kinase inhibitor	AXL | FLT3 | KIT | MET | MST1R | PDGFRA | RAD51 | RET	Non-epigenetic	Non-epigenetic
Anastrozole	2187	Launched	Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM	aromatase inhibitor	CYP19A1	Non-epigenetic	Non-epigenetic
Anisomycin	253602	Preclinical	Anisomycin is a potent protein synthesis inhibitor which interferes with protein and DNA synthesis by inhibiting peptidyl transferase or the 80S ribosome system. Anisomycin is a JNK activator, which increases phospho-JNK. Anisomycin is a bacterial antibiotic	dna synthesis inhibitor	NHP2L1 | RPL10L | RPL11 | RPL13A | RPL15 | RPL19 | RPL23 | RPL23A | RPL26L1 | RPL3 | RPL37 | RPL8 | RSL24D1	Non-epigenetic	Non-epigenetic
AP1903	16135625	Phase 1/Phase 2	Rimiducid (AP1903) is a dimerizer agent that acts by cross-linking the FKBP domains. Rimiducid (AP1903) dimerizes the Caspase 9 suicide switch and rapidly induces apoptosis	FKBP domain cross linker	MTOR	Non-epigenetic	Non-epigenetic
Apremilast	11561674	Launched	Apremilast (CC-10004) is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM	phosphodiesterase inhibitor	PDE4A | PDE4B | PDE4C | PDE4D | TNF | TNFRSF1A	Non-epigenetic	Non-epigenetic
Arachidonyl	5311006	Preclinical	Dual fatty acid amide hydrolase (FAAH) inhibitor/TRPV1 antagonist (IC50 values are 5.6μM and 37-40 nM for FAAH and TRPV1 respectively). Inactive at cPLA2, CB1 or 5-HT receptors. Displays strong analgesic activity against both acute and chronicperipheral pain.	faah inhibitor | trpv1 antagonist	FAAH | TRPV1	Non-epigenetic	Non-epigenetic
ARD-61	154704831	Preclinical	(PROTAC) Androgen Receptor Degrader	androgen receptor degrader	AR	Non-epigenetic	Non-epigenetic
ARD-61b	154704831	Preclinical	(PROTAC) Androgen Receptor Degrader	androgen receptor degrader	AR	Non-epigenetic	Non-epigenetic
ARN509	24872560	Launched	Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM	androgen receptor antagonist	AR	Non-epigenetic	Non-epigenetic
Arsenic	5359596	Preclinical	Arsenic trioxide is a chemotherapeutic agent of idiopathic function used to treat leukemia that is unresponsive to first line agents. It is suspected that arsenic trisulfide induces cancer cells to undergo apoptosis. In general, arsenic is known to be a naturally toxic substance capable of eliciting a variety of dangerous adverse effects. The enzyme thioredoxin reductase has recently been identified as a target for arsenic trioxide	apoptosis stimulant		Non-epigenetic	Non-epigenetic
ASLAN003	24986824	Preclinical	A novel, potent Dihydroorotate Dehydrogenase (DHODH) Inhibitor	dhodh inhibitor	DHODH	Non-epigenetic	Non-epigenetic
Aspirin	2244	Launched	Aspirin (Acetylsalicylic Acid) is an orally active, potent and irreversible inhibitor of cyclooxygenase COX-1 and COX-2, with IC50 values of 5 and 210 μg/mL, respectively. Aspirin induces apoptosis. Aspirin inhibits the activation of NF-κB. Aspirin also inhibits platelet prostaglandin synthetase, and can prevent coronary artery and cerebrovascular thrombosis	cyclooxygenase inhibitor	AKR1C1 | ASIC3 | EDNRA | HSPA5 | IKBKB | NFKB1 | NFKB2 | NFKBIA | PRKAA1 | PRKAA2 | PRKAB1 | PRKAB2 | PRKAG1 | PRKAG2 | PRKAG3 | PTGS1 | PTGS2 | RPS6KA3 | TP53	Non-epigenetic	Non-epigenetic
Astemizole	2247	Withdrawn	Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects	histamine receptor antagonist	CYP2J2 | CYP3A5 | HRH1 | KCNH1 | KCNH2	Non-epigenetic	Non-epigenetic
AT-101	3503	Phase 2	(R)-(-)-Gossypol (AT-101) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively	bcl inhibitor | mcl1 inhibitor	BCL2 | BCL2L1 | BCL2L2 | CTGF | EGF | MCL1	Non-epigenetic	Non-epigenetic
AT9283	135398495	Phase 2	AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo	aurora kinase inhibitor | jak inhibitor	ABL1 | AURKA | AURKB | BCR | FLT3 | JAK2 | JAK3 | RPS6KA6 | STK17A	Non-epigenetic	Non-epigenetic
ATN161	9960285	Phase 2	ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model	integrin antagonist	ITGA5 | ITGAV | ITGB1 | ITGB3 | ITGB5	Non-epigenetic	Non-epigenetic
Atrasentan	159594	Phase 3	Atrasentan (ABT-627) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA	endothelin receptor antagonist	EDNRA	Non-epigenetic	Non-epigenetic
Atrovastatin	60823	Launched	Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids. Atorvastatin inhibits human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively.	hmgcr inhibitor	AHR | CYP3A5 | DPP4 | FASLG | HMGCR	Non-epigenetic	Non-epigenetic
Auranofin	24199313	Preclinical	Auranofin (SKF-39162) is a thioredoxin reductase (TrxR) inhibitor with an IC50 of 0.2 μM. Auranofin exhibits antiviral activity against SARS-CoV21, with a CC50 of 4.2 μM for monkey kidney Vero E6 cells.	thioredoxin reductase (trxr) inhibitor	TrxR	Non-epigenetic	Non-epigenetic
AUY922	135539077	Phase 2	Luminespib (VER-52296) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.	hsp inhibitor	HSP90AA1 | HSP90AB1	Non-epigenetic	Non-epigenetic
Avadomide	24967599	Phase 2	New chemical entity termed pleiotropic pathway modifier, is a novel agent for Diffuse large B-cell lymphoma (DLBCL) with antitumor and immunomodulatory activity. Its molecular target is the protein cereblon (CRBN), a substrate receptor of the cullin ring E3 ubiquitin ligase complex CRL4-CRBN	antitumor agent	CRBN	Non-epigenetic	Non-epigenetic
AVL292	59174488	Phase 2	Spebrutinib (AVL-292; CC-292) is a covalent, orally active, and highly selective with an IC50 of 0.5 nM	bruton's tyrosine kinase (btk) inhibitor	BTK | EGFR | ITK | JAK3 | YES1	Non-epigenetic	Non-epigenetic
AVN944	9918559	Phase 2	AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) researc	inosine monophosphate dehydrogenase inhibitor	IMPDH1 | IMPDH2	Non-epigenetic	Non-epigenetic
Axitinib	6450551	Launched	Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively	pdgfr tyrosine kinase receptor inhibitor | vegfr inhibitor	CSF1 | CYP2C19 | CYP3A5 | FLT1 | FLT4 | KDR | KIT | PDGFRB | PLK4	Non-epigenetic	Non-epigenetic
AZ12419304	16750158	Preclinical		ras-raf-mek inhibitor	MEK | RAF | RAS	Non-epigenetic	Non-epigenetic
AZ12456623		Preclinical		mapk inhibitor	MAPK	Non-epigenetic	Non-epigenetic
AZ12609721		Preclinical	Ephrin receptor B4 (EphB4) tyrosine kinase inhibitor	ephb4 inhibitor	EphB4	Non-epigenetic	Non-epigenetic
AZ12823138		Preclinical		braf inhibitor	BRAF	Non-epigenetic	Non-epigenetic
AZ5576	53373586	Preclinical	AZ5576 is a potent and highly selective CDK9 inhibitor. AZ5576 can be used for hematological Malignancy research.	cdk inhibitor	CDK9	Non-epigenetic	Non-epigenetic
AZ5576 + DBK-1154		Preclinical	Combination: AZ5576 is a potent and highly selective CDK9 inhibitor. AZ5576 can be used for hematological Malignancy research and SMAP-2 (DT-1154) is an orally active protein phosphatase 2A (PP2A) activator, with anti-cancer activity.	kinase inhibitor | pp2a-activator	CDK9 | PP2A	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Azacitidine	9444	Launched	Nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.	dna methyltransferase inhibitor	DNMT1 | DNMT3A	Writer	DNMTi
Azacitidine + Carboplatin		Launched	Combination: Azacitidine + Carboplatin	alkylating agent | dna inhibitor | dna methyltransferase inhibitor	DNMT1 | DNMT3A | DNMT3B	Writer | Non-epigenetic	DNMTi | Non-epigenetic
Azacitidine + GSK2879552		Launched	Combination: (Azacitidine) Nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy. (GSK2879552) Lysine-specific histone demethylase 1 (LSD) inhibitor	dna methyltransferase inhibitor | histone lysine demethylase inhibitor	DNMT1 | KDM1A	Eraser | Writer	DNMTi | HDMi
Azacitidine + Panobinostat		Launched	Combination: (Azacitidine) Nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy. (Panobinostat) Broad-spectrum HDAC inhibitor with IC50 of 5 nM. Phase 3.	dna methyltransferase inhibitor | hdac inhibitor	DNMT1 | HDAC1 | HDAC2 | HDAC3 | HDAC4 | HDAC6 | HDAC7 | HDAC8 | HDAC9	Eraser | Writer	DNMTi | HDACi
Azacitidine + Retinoic Acid		Launched | Launched	Combination: Azacitidine + Retinoic acid	dna methyltransferase inhibitor | retinoid receptor agonist | retinoid receptor ligand	DNMT1 | DNMT3A | ALDH1A1 | ALDH1A2 | GPRC5A | NR0B1 | NR2C2 | PPARD | RARA | RARB | RARG | RARRES1 | RORB | RORC | RXRB | RXRG	Writer | Non-epigenetic	DNMTi | Non-epigenetic
Azathioprine	2265	Launched	Azathioprine(BW 57-322) is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.	dehydrogenase inhibitor	HPRT1 | IMPDH1 | PPAT	Non-epigenetic	Non-epigenetic
AZD1480	16659841	Phase 1	AZD-1480 is an ATP-competitive inhibitor of JAK1 and JAK2 with IC50s of 1.3 nM and <0.4 nM, respectively	jak inhibitor	JAK1 | JAK2 | JAK3	Non-epigenetic	Non-epigenetic
AZD2014	25262792	Phase 2	Vistusertib (AZD2014) is an ATP competitive mTOR inhibitor with an IC50 of 2.81 nM. AZD2014 inhibits both mTORC1 and mTORC2 complexes	mtor inhibitor	MTOR	Non-epigenetic	Non-epigenetic
AZD5069	56645576	Phase 2	AZD-5069 is a potent CXCR2 chemokine receptor antagonist, used for caner treatment	cc chemokine receptor antagonist	CXCR2	Non-epigenetic	Non-epigenetic
AZD5153	118693659	Phase 1	A potent, selective, and orally available BET/BRD4 bromodomain inhibitor possessing a bivalent binding mode. Unlike previously described monovalent inhibitors, AZD5153 ligates two bromodomains in BRD4 simultaneously	bromodomain inhibitor	BRD4 | E2F | MTOR | MYC	Reader	PAHi
AZD5363	25227436	Phase 3	Capivasertib (AZD5363) is an orally active and potent pan-AKT kinase inhibitor with IC50 of 3, 7 and 7 nM for Akt1,Akt2 and Akt3, respectively.	akt inhibitor	AKT1 | AKT2 | AKT3	Non-epigenetic	Non-epigenetic
AZD6482	44137675	Phase 1	PI3Kβ inhibitor with IC50 of 10 nM, 8-, 87- and 109-fold more selective to PI3Kβ than PI3Kδ, PI3Kα and PI3Kγ. Phase 1.	pi3k inhibitor	PIK3CA | PIK3CB | PIK3CD | PIK3CG	Non-epigenetic	Non-epigenetic
AZD7762	11152667	Phase 1	Inhibitor of Chk1 with IC50 of 5nM. It is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck. Phase 1.	chk inhibitor	CHEK1 | CHEK2	Non-epigenetic	Non-epigenetic
AZD8055	25262965	Phase 1	ATP-competitive mTOR inhibitor with IC50 of 0.8 nM with excellent selectivity (1,000-fold) against PI3K isoforms and ATM/DNA-PK. Phase 1	mtor inhibitor	MTOR	Non-epigenetic	Non-epigenetic
AZD8542	53344810	Preclinical	Smoothened (SMO), frizzled family receptor antagonist	smoothened antagonist	SMO	Non-epigenetic	Non-epigenetic
Bafetinib	11387605	Phase 2	Dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. Phase 2.	bcr-abl kinase inhibitor | lyn tyrosine kinase inhibitor	ABL1 | BCR | FYN | LYN	Non-epigenetic	Non-epigenetic
Banoxantrone	9955116	Phase 1/Phase 2	Banoxantrone-d12 (dihydrochloride) is the deuterium labeled Banoxantrone dihydrochloride. Banoxantrone is a novel bioreductive agent that can be reduced to a stable, DNA-affinic compound AQ4, which is a potent topoisomerase II inhibitor	topoisomerase inhibitor	TOP2A | TOP2B	Non-epigenetic	Non-epigenetic
Bardoxolone methyl	400769	Phase 3	IKK inhibitor, showing potent proapoptotic and anti-inflammatory activities. Phase 3	nuclear factor erythroid derived, like (nrf2) activator	BCL2 | CHUK | GSR | HMOX1 | HMOX2 | NFE2L2 | PPARG | STAT3	Non-epigenetic	Non-epigenetic
Baricitinib	44205240	Launched	Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively	jak inhibitor	JAK1 | JAK2	Non-epigenetic	Non-epigenetic
Bax channel blocker	2729026	Preclinical	Allosteric inhibitor of Bax channel activation. Binds inactive Bax\r\nat allosteric site and inhibits tBID-mediated Bax activation (IC50 =\r\n3.3 µM). Selectively inhibits Bax-dependent apoptosis. Potent\r\ninhibitor of Bax-mediated mitochondrial cytochrome c release\r\n(IC50 = 0.52 µM).	bax channel inhibitor	BAX	Non-epigenetic	Non-epigenetic
Bay 11-7085	5353432	Preclinical	BAY 11-7085 (BAY 11-7083) is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC50 of 10 μM	nfkb pathway inhibitor	NFKBIA	Non-epigenetic	Non-epigenetic
Bay 11-7821	5353431	Preclinical	BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells	nfkb pathway inhibitor	RELA	Non-epigenetic	Non-epigenetic
BAY 1436032	118310260	Phase 1	Highly selective, potent and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). It is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displays potent inhibition of 2-HG release (nanomolar range) in patient derived and engineered cell lines expressing different IDH1 mutants.	isocitrate dehydrogenase inhibitor	IDH1	Non-epigenetic	Non-epigenetic
BAY 1436032 + Azacitidine		Phase 1 | Launched	Combination: Highly selective, potent and orally available inhibitor of mutant Isocitrate Dehydrogenase 1 (mIDH1). It is a double-digit nanomolar and selective pan-inhibitor of the enzymatic activity of various IDH1-R132X mutants in vitro and displays potent inhibition of 2-HG release (nanomolar range) in patient derived and engineered cell lines expressing different IDH1 mutants. (Azacitidine) Nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.	dna methyltransferase inhibitor | isocitrate dehydrogenase inhibitor	DNMT1 | DNMT3A | IDH1	Writer | Non-epigenetic	DNMTi | Non-epigenetic
Belinostat	6918638	Launched	HDAC inhibitor with IC50 of 27 nM, with activity demonstrated in cisplatin-resistant tumors. Phase 1/2	hdac inhibitor	HDAC1 | HDAC10 | HDAC11 | HDAC2 | HDAC3 | HDAC4 | HDAC5 | HDAC6 | HDAC7 | HDAC8 | HDAC9	Eraser	HDACi
Bendamustine	65628	Launched	Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties	dna inhibitor		Non-epigenetic	Non-epigenetic
Benserazide hydrochloride	26964	Launched	Benserazide hydrochloride (Serazide) is commonly used in Parkinson's disease and is an inhibitor of peripheral aromatic L-amino acid decarboxylase (AADC)	dopa decarboxylase inhibitor	DDC	Non-epigenetic	Non-epigenetic
Berberine	2353	Launched	Berberine chloride is an alkaloid that acts as an antibiotic. Berberine chloride induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties	ldl receptor activator	ACHE | CYP2C19 | CYP2E1 | LDLR | PTPN1	Non-epigenetic	Non-epigenetic
beta-Lapachone	3885	Phase 2	β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression	topoisomerase inhibitor	E2F1 | IDO1 | TDO2 | TOP1	Non-epigenetic	Non-epigenetic
Bexarotene	82146	Launched	Retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma.	retinoid receptor agonist	ABCA1 | CYP2C8 | CYP3A4 | RXRA | RXRB | RXRG	Non-epigenetic	Non-epigenetic
BGJ398	53235510	Phase 3	FGFR inhibitor for FGFR1/2/3 with IC50 of 0.9 nM/1.4 nM/1 nM in cell-free assays, >40-fold selective for FGFR versus FGFR4 and VEGFR2, and little activity to Abl, Fyn,Kit, Lck, Lyn and Yes. Phase 2	fgfr inhibitor	FGFR1 | FGFR2 | FGFR3 | FGFR4 | KDR	Non-epigenetic	Non-epigenetic
BI-2536	11364421	Phase 2	Plk1 inhibitor with IC50 of 0.83 nM in a cell-free assay. It shows 4- and 11-fold greater selectivity against Plk2 and Plk3. Phase 2	plk inhibitor	BRD4 | PLK1 | PLK2 | PLK3	Reader	PAHi
BI-7273	118796358	Preclinical	BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.	bromodomain inhibitor	BRD7 | BRD9	Reader	PAHi
BI-87G3	44156976	Preclinical	BI-87G3 is a cell-permeable, potent and selective competitive inhibitor of the c-Jun N-terminal kinase (JNK). BI-87G3 is a JNK inhibitor that targets the JIP-JNK interaction site.	jnk inhibitor	JNK	Non-epigenetic	Non-epigenetic
BI00894999	76072013	Preclinical	Selective BET inhibitor	bromodomain inhibitor	BRD2 | BRD3 | BRD4 | BRDT	Reader	PAHi
BI00894999 + EX00101218		Preclinical	Combination: Selective BET inhibitors	aurora kinase inhibitor | bromodomain inhibitor	AURKA | AURKB | AURKC | BRD2 | BRD3 | BRD4	Reader | Reader	PAHi | PAHi
BI00894999 + Volasertib		Preclinical	Combination: (BI00894999) Selective BET inhibitor and (Volasertib) Highly potent Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM, as well as the two closely related kinases PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively	bromodomain inhibitor | plk inhibitor	BRD2 | BRD3 | BRD4 | PLK1	Reader | Reader	PAHi | PAHi
BI2536	11364421	Phase 2	BI 2536 is a dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively. BI-2536 suppresses IFNB (encoding IFN-β) gene transcription.	plk inhibitor	BRD4 | PLK1 | PLK2 | PLK3	Reader	PAHi
BI8622	138377590	Preclinical	HUWE1 ubiquitin ligase inhibitor	huwe1 inhibitor	HUWE1	Non-epigenetic	Non-epigenetic
BI8622 + Doxycycline		Preclinical	Combination: (BI8622) HUWE1 ubiquitin ligase inhibitor and (Doxycycline) an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.	bacterial 30s ribosomal subunit inhibitor | huwe1 inhibitor | metalloproteinase inhibitor	HUWE1 | MMP1 | MMP8	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
BIBU 1361 dihydrochloride	46861539	Preclinical	BIBU1361 induces apoptosis and inhibits autophagy. BIBU1361 inhibits pro-survival pathways Akt/mTOR and gp130/JAK/STAT3, and decreased levels of pro-inflammatory cytokine IL-6	akt inhibitor	AKT1 | AKT2 | AKT3	Non-epigenetic	Non-epigenetic
Bicalutamide	2375	Launched	Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer	androgen receptor antagonist	AR | CYP2C19	Non-epigenetic	Non-epigenetic
BIIB021	16736529	Phase 2	BIIB021 (CNF2024) is an orally active, fully synthetic inhibitor of HSP90 with a Ki and an EC50 of 1.7 nM and 38 nM, respectively	hsp inhibitor	AOX1 | HSP90AA1	Non-epigenetic	Non-epigenetic
Binimetinib	10288191	Launched	Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM	mek inhibitor	IL1R2 | IL6R | MAP2K1 | MAP2K2 | TNFRSF1A	Non-epigenetic	Non-epigenetic
BIO	448949	Preclinical	Inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor.	glycogen synthase kinase inhibitor | lipoxygenase inhibitor	ALOX5 | GSK3A | GSK3B	Non-epigenetic	Non-epigenetic
Birabresib	9936746	Phase 1/Phase 2	Birabresib (OTX-015) is a potent bromodomain (BRD2/3/4) inhibitor with IC50s ranging from 92 to 112 nM	bromodomain inhibitor	BRD2 | BRD3 | BRD4 | SELE | VCAM1	Reader	PAHi
Birinapant	49836020	Phase 2	Birinapant (TL32711), a bivalent Smac mimetic, is a potent antagonist for XIAP and cIAP1 with Kds of 45 nM and less than 1 nM, respectively. Birinapant (TL32711) induces the autoubiquitylation and proteasomal degradation of cIAP1 and cIAP2 in intact cells, which results in formation of a RIPK1: caspase-8 complex, caspase-8 activation, and induction of tumor cell death. Birinapant (TL32711) targets TRAF2-associated cIAPs and abrogates TNF-induced NF-κB activation	xiap inhibitor	BIRC2 | BIRC3 | XIAP	Non-epigenetic	Non-epigenetic
BIX-01294	25150857	Preclinical	BIX-01294 is an inhibitor of G9a Histone Methyltransferase with an IC50 of 1.9 μM.	histone lysine methyltransferase inhibitor	EHMT1 | EHMT2	Writer	HMTi
BIX01294	25150857	Preclinical	BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells	histone lysine methyltransferase inhibitor	EHMT1 | EHMT2	Writer	HMTi
BKM120	16654980	Phase 3	Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.	pi3k inhibitor	PIK3CA | PIK3CG	Non-epigenetic	Non-epigenetic
Bleomycin	5360373	Launched	Bleomycin hydrochloride is a DNA synthesis inhibitor. Bleomycin hydrochloride is a DNA damaging agent. Bleomycin hydrochloride is an antitumor antibiotic	dna damage inducer | dna synthesis inhibitor		Non-epigenetic	Non-epigenetic
BLM-KO		N/A	BLM-knock Out	N/A	BLM	Non-epigenetic	Non-epigenetic
BMI-1 OE		N/A	BMI-1 Overexpression	N/A	BMI1	Non-epigenetic	Non-epigenetic
BMP4		Preclinical		bone morphogenic proteins	BMP4	Non-epigenetic	Non-epigenetic
BMP4 + Temozolomide		Preclinical	Combination: BMP4 + Temozolomide	bone morphogenic proteins | dna alkylating agent	BMPF | MGMT | TOP2A	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
BMS-754807	24785538	Phase 2	Reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM, less potent to Met, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKCetc. Phase 1/2.	igf-1 inhibitor	AKT1 | IGF1R	Non-epigenetic	Non-epigenetic
BNTX maleate salt hydrate	51371157	Preclinical	BNTX, a selective nonpeptide σ1 opioid receptor (DOR1) antagonist, is used in σ opioid receptor research to help differentiate and characterized the function and role of the σ1 opioid receptor versus other σ opioid receptor subtypes.[1] BNTX was used to help define the role of σ1 opioid receptors in neurological processes such as anxiety. It was used to help define the role of σ opioid receptors in myocardial infarct development and size	delta 1 opioid antagonist	DOR1	Non-epigenetic	Non-epigenetic
Bortezomib	387447	Launched	Potent 20S proteasome inhibitor with Ki of 0.6 nM	nfkb pathway inhibitor | proteasome inhibitor	CASP3 | CYP2C19 | NFKB1 | PSMA1 | PSMA2 | PSMA3 | PSMA4 | PSMA5 | PSMA6 | PSMA7 | PSMA8 | PSMB1 | PSMB10 | PSMB11 | PSMB2 | PSMB3 | PSMB4 | PSMB5 | PSMB6 | PSMB7 | PSMB8 | PSMB9 | PSMD1 | PSMD2 | RELA	Non-epigenetic	Non-epigenetic
Bosentan	104865	Launched	Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively	endothelin receptor antagonist	ABCB1 | CYP2C19 | CYP3A4 | EDNRA | EDNRB	Non-epigenetic	Non-epigenetic
Bosutinib	5328940	Launched	Bosutinib is an orally active Src/Abl tyrosine kinase inhibitor with IC50 of 1.2 nM and 1 nM, respectively	abl kinase inhibitor | bcr-abl kinase inhibitor | src inhibitor	ABL1 | BCR | CAMK1D | CAMK2G | CDK2 | FRK | FYN | HCK | LYN | MAP2K1 | MAP2K2 | MAP3K2 | MAP4K5 | SRC | STK10 | STK24 | STK4 | TNK2 | TXK	Non-epigenetic	Non-epigenetic
BRAFi		Preclinical	BRAF inhibitor	raf inhibitor	BRAF	Non-epigenetic	Non-epigenetic
Brefeldin A	5287620	Preclinical	Brefeldin A is a lactone antibiotic and ATPase inhibitor for protein transport with IC50 of 0.2μM in HCT 116 cells, induces cancer cell differentiation and apoptosis	protein synthesis inhibitor	ARF1 | ARFGEF1 | ARFGEF2 | CYTH2 | GBF1	Non-epigenetic	Non-epigenetic
Brentuximab Vedotin		Phase 2	Brentuximab vedotin, sold under the brand name Adcetris, is an antibody-drug conjugate medication used to treat relapsed or refractory Hodgkin lymphoma (HL) and systemic anaplastic large cell lymphoma (ALCL), a type of T cell non-Hodgkin lymphoma. It selectively targets tumor cells expressing the CD30 antigen, a defining marker of Hodgkin lymphoma and ALCL.	antimitotic agent	TNFRSF10B | TPPP	Non-epigenetic	Non-epigenetic
Brigatinib	68165256	Launched	Brigatinib (AP-26113) is a highly potent, selective and orally active ALK inhibitor, with an IC50 of 0.6 nM. Brigatinib can be used for research of NSCLC	alk tyrosine kinase receptor inhibitor | egfr inhibitor	ALK | EGFR | IGF1R | ROS1	Non-epigenetic	Non-epigenetic
Brivanib	11234052	Phase 3	ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3.	fgfr inhibitor | vegfr inhibitor	CYP3A4 | FGFR1 | FGFR2 | FGFR3 | FLT1 | FLT4 | KCNH2 | KDR	Non-epigenetic	Non-epigenetic
BRM011	145992229	Preclinical	BRM011 and its structurally related analogs display cellular activity in modulating BRM-dependent gene expression and inducing growth inhibition in BRG1-mutant lung cancer models.	atp synthase inhibitor	SMARCA2 | SMARCA4	Remodeler	Non-epigenetic
Bromoacetyl alprenolol menthane	11957482	Launched	Alprenolol ((RS)-Alprenolol; dl-Alprenolol) is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent	adrenergic receptor antagonist	ADRB1 | ADRB2	Non-epigenetic	Non-epigenetic
BSJ-116	155235839	Preclinical	CDK12 degrader	protac	CDK12	Non-epigenetic	Non-epigenetic
BSJ-4-23	155235827	Preclinical	CDK12 degrader	protac	CDK12	Non-epigenetic	Non-epigenetic
BSJ-4-23NC		Preclinical	CDK12 degrader negative control	protac (nonfunctional)	CDK12	Non-epigenetic	Non-epigenetic
Buparlisib	16654980	Phase 3	PI3K inhibitor of p110α/β/δ/γ with IC50 of 52 nM/166 nM/116 nM/262 nM, respectively. Reduced potency against VPS34, mTOR, DNAPK, with little activity to PI4Kβ. Phase 1/2	pi3k inhibitor	PIK3CA | PIK3CG	Non-epigenetic	Non-epigenetic
Busulfan	2478	Launched	Cell cycle non-specific alkylating antineoplastic agent. Busulfan induces apoptosis.	dna inhibitor		Non-epigenetic	Non-epigenetic
Busulfan + Cyclophosphamide		Launched | Launched	Combination: (Busulfan) Cell cycle non-specific alkylating antineoplastic agent. Busulfan induces apoptosis and (Cyclophoshamide) a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic activity, a immunosuppressant.	dna alkylating agent | dna inhibitor	BCL2 | CYP2A6 | CYP2B6 | CYP2C18 | CYP2C19 | CYP2C8 | CYP2C9 | CYP2D6 | CYP3A4 | CYP3A5 | CYP3A7 | LGALS1	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
C646	1285941	Preclinical	C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.	histone acetyltransferase inhibitor	EP300	Writer	HATi
Cabazitaxel	9854073	Launched	Cabazitaxel is a semi-synthetic derivative of the natural taxoid 10-deacetylbaccatin III with potential antineoplastic activity	microtubule inhibitor	CYP2C8 | CYP3A5 | SLCO1B3 | TUBA1A | TUBA1B | TUBA1C | TUBA3C | TUBA3D | TUBA3E | TUBA4A | TUBB | TUBB1 | TUBB2A | TUBB2B | TUBB3 | TUBB4A | TUBB4B | TUBB6 | TUBB8	Non-epigenetic	Non-epigenetic
Cabergoline	54746	Launched	Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively)	dopamine receptor agonist	ADRA1A | ADRA1B | ADRA1D | ADRA2A | ADRA2B | ADRA2C | ADRB1 | ADRB2 | DRD1 | DRD2 | DRD3 | DRD4 | DRD5 | HTR1A | HTR1B | HTR1D | HTR2A | HTR2B | HTR2C | HTR7 | PRL	Non-epigenetic	Non-epigenetic
Cabozantinib	25102847	Launched	Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis	ret tyrosine kinase inhibitor | vegfr inhibitor	CYP2C19 | FLT3 | KDR | KIT | MET | RET | TEK	Non-epigenetic	Non-epigenetic
Calcimycin	11957499	Preclinical	Calcimycin (A-23187) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin induces Ca2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin induces apoptosis	other antibiotic		Non-epigenetic	Non-epigenetic
Calcitriol	5280453	Launched	Calcitriol is the most active metabolite of vitamin D and also a vitamin D receptor (VDR) agonist.	vitamin d receptor agonist	CYP3A5 | VDR	Non-epigenetic	Non-epigenetic
Calmidazolium chloride	644274	Preclinical	Calmidazolium chloride (R 24571) is a calmodulin antagonist, antagonizing CaM-dependent phosphodiesterase and calmodulin-induced activation of erythrocyte Ca2+-transporting ATPase with IC50s of 0.15 and 0.35 μM, respectively. Also in anti-cancer research. Calmidazolium binds to calmodulin with a Kd of 3 nM	calmodulin antagonist	CALM1	Non-epigenetic	Non-epigenetic
Camptothecin	24360	Phase 3	Camptothecin (CPT) effectively inhibits the interferon-β (IFN-β)–driven transcription from chromatinized templates	topoisomerase inhibitor	HIF1A | TOP1	Non-epigenetic	Non-epigenetic
Canertinib	156414	Phase 3	Canertinib (CI-1033;PD-183805) is a potent and irreversible EGFR inhibitor; inhibits cellular EGFR and ErbB2 autophosphorylation with IC50s of 7.4 and 9 nM. Canertinib is active against vaccinia virus respiratory infection in mice	egfr inhibitor	AKT1 | EGFR | ERBB2 | ERBB4	Non-epigenetic	Non-epigenetic
Cantharidin	5944	Launched	(Rac)-Norcantharidin ((Rac)-NCTD) is the isoform of Norcantharidin, which is a synthetic and demethylated anticancer agent derived from Cantharidin (HY-N0209). Norcantharidin has lighter side effects and stronger bioactivity than Cantharidin. And Norcantharidin inhibits cell proliferation, migration and metastasis, and causes apoptosis and autophagy	protein phosphatase inhibitor		Non-epigenetic	Non-epigenetic
Capecitabine	60953	Launched	Capecitabine is an oral proagent that is converted to its active metabolite, 5-FU, by thymidine phosphorylase	dna synthesis inhibitor | thymidylate synthase inhibitor	DPYD | TYMS	Non-epigenetic	Non-epigenetic
Capmatinib	25145656	Phase 3	ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM in a cell-free assay, inactive against RONβ, as well as EGFR and HER-3. Phase 1.	c-met inhibitor	MET	Non-epigenetic	Non-epigenetic
Carboplatin	10339178	Launched	DNA synthesis inhibitor by binding to DNA and interfering with the cell's repair mechanism in A2780, SKOV-3, IGROV-1, and HX62 cells.	dna alkylating agent | dna synthesis inhibitor		Non-epigenetic	Non-epigenetic
Carfilzomib	11556711	Launched	Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis	proteasome inhibitor	PSMA1 | PSMA2 | PSMA3 | PSMA4 | PSMA5 | PSMA6 | PSMA7 | PSMA8 | PSMB1 | PSMB10 | PSMB11 | PSMB2 | PSMB3 | PSMB4 | PSMB5 | PSMB6 | PSMB7 | PSMB8 | PSMB9	Non-epigenetic	Non-epigenetic
Carmustine	2578	Launched	Carmustine is an antitumor chemotherapeutic agent, which works by akylating DNA and RNA	dna alkylating agent | dna inhibitor	GSR | TXNRD1 | TXNRD2	Non-epigenetic	Non-epigenetic
cas9 CDK11B-1346		N/A	cas9 KO of CDK11B-1346	cas9 editing	CDK11B	Non-epigenetic	Non-epigenetic
cas9 CDK11B-1347		N/A	cas9 KO of CDK11B-1347	cas9 editing	CDK11B	Non-epigenetic	Non-epigenetic
cas9 CDK11B-1348		N/A	cas9 KO of CDK11B-1348	cas9 editing	CDK11B	Non-epigenetic	Non-epigenetic
cas9 CDK11B-1349		N/A	cas9 KO of CDK11B-1349	cas9 editing	CDK11B	Non-epigenetic	Non-epigenetic
CAY10566	16732433	Preclinical	CAY10566 is a potent, orally bioavailable and selective stearoyl-CoA desaturase1 (SCD1) inhibitor with IC50s of 4.5 and 26 nM in mouse and human enzymatic assays, respectively. CAY10566 also shows excellent cellular activity in blocking the conversion of saturated long-chain fatty acid-CoAs (LCFA-CoAs) to monounsaturated LCFA-CoAs in HepG2 cells (IC50=7.9 nM or 6.8 nM).	stearoyl-coa desaturase1 (scd1) inhibitor	SCD1	Non-epigenetic	Non-epigenetic
CAY10618	44819697	Preclinical	Inhibitor of NAMPT (IC50= 3.0 nM). It induces cell death in the neuroblastoma cell line SH-SY5Y with an IC50 value of 3.8 nM through a process that appears to involve autophagy.	nampt inhibitor	NAMPT	Non-epigenetic	Non-epigenetic
CC223	58298316	Phase 2	Onatasertib (CC-223) is a potent, selective, and orally bioavailable inhibitor of mTOR kinase, with an IC50 value for mTOR kinase of 16 nM. Onatasertib inhibits both mTORC1 and mTORC2	mtor inhibitor	MTOR	Non-epigenetic	Non-epigenetic
CCG-222740	121317937	Preclinical	CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.	mrtf pathway inhibitor	MRTF	Non-epigenetic	Non-epigenetic
CCT128930	17751819	Preclinical	CCT128930 is a ATP-competitive and selective inhibitor of AKT (IC50=6 nM for AKT2). CCT128930 has 28-fold selectivity over the closely related PKA kinase (IC50=168 nM) through the targeting of Met282 of AKT (Met173 of PKA-AKT chimera), as well as 20-fold selectivity over p70S6K (IC50=120 nM). Antitumor activity	akt inhibitor	ROCK1 | ROCK2	Non-epigenetic	Non-epigenetic
CD-437	135411	Preclinical	Synthetic retinoid that is an RARγ-selective agonist. Displays RARγ-dependent and -independent effects on differentiation and apoptosis.	retinoid receptor agonist	RARG	Non-epigenetic	Non-epigenetic
Cdk/Crk Inhibitor	135473382	Preclinical	The Cdk/Crk Inhibitor, also referenced under CAS 784211-09-2, controls the biological activity of Cdk/Crk. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications	cdk inhibitor	CDK1 | CDK2 | CDK4 | CDK6	Non-epigenetic	Non-epigenetic
CDK13 Mutation Impacting PAXT		N/A	Cyclin Dependent Kinase 13 (CDK13) is mutated in melanoma and patient-mutated CDK13 accelerates zebrafish melanoma. CDK13 mutation causes aberrant RNA stabilization. CDK13 is required for ZC3H14 phosphorylation, which is necessary and sufficient to promote nuclear RNA degradation. Mutant CDK13 fails to activate nuclear RNA surveillance, causing aberrant protein-coding transcripts to be stabilized and translated. Forced aberrant RNA expression accelerates melanoma in zebrafish. We find recurrent mutations in genes encoding nuclear RNA surveillance components in many malignancies, establishing nuclear RNA surveillance as a tumor-suppressive pathway. Activating nuclear RNA surveillance is crucial to avoid accumulation of aberrant RNAs and their ensuing consequences in development and disease.	N/A	CDK13 | PAXT	Non-epigenetic	Non-epigenetic
Cediranib	9933475	Phase 3	Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively	kit inhibitor | vegfr inhibitor	CSF1R | FLT1 | FLT3 | FLT4 | KDR | KIT | PDGFRA | PDGFRB	Non-epigenetic	Non-epigenetic
Ceritinib	57379345	Launched	ALK inhibitor with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Phase 2.	alk tyrosine kinase receptor inhibitor	ALK | FLT3 | IGF1R | INSR | TSSK1B	Non-epigenetic	Non-epigenetic
Cerulenin	5282054	Launched	Irreversibly binds to fatty acid synthase, specifically b-ketoacyl-acyl carrier protein synthase (FabH, FabB and FabF condensation enzymes). A number of tumor cells and cell lines have been observed to have highly upregulated expression and activity of fatty acid synthase (FAS). Inhibition of FAS by cerulenin leads to cytotoxicity and apoptosis in human cancer cell lines, an effect believed to be mediated by the accumulation of malonyl-coenzyme A in cells with an upregulated FAS pathway	fatty acid synthase inhibitor	FASN	Non-epigenetic	Non-epigenetic
CGK733	6605258	Preclinical	CGK733 is a potent ATM/ATR inhibitor, used for the research of cancer	atm kinase inhibitor | atr kinase inhibitor	ATM | ATR	Non-epigenetic	Non-epigenetic
CGP 71683 hydrochloride	9849276	Preclinical	CGP71683 hydrochloride is a competitive neuropeptide Y5 receptor antagonist with a Ki of 1.3 nM, and shows no obvious activity at Y1 receptor (Ki, >4000 nM) and Y2 receptor (Ki, 200 nM) in cell membranes	y5 receptor antagonist	Y5	Non-epigenetic	Non-epigenetic
CGP 74514A hydrochloride	11957495	Preclinical	CGP-74514A hydrochloride is a potent CDK1 inhibitor with IC50 of 25 nM; induces caspase-9 activation and PARP degradation, mediates apoptosis in U937 cells; increases p21(CIP1) expression, p27(KIP1) degradation, diminished E2F1 expression, and dephosphorylation of p34(CDC2).	cdk inhibitor	CDK1	Non-epigenetic	Non-epigenetic
Chelerythrine chloride	72311	Preclinical	Chelerythrine chloride is a potent, cell-permeable inhibitor of protein kinase C, with an IC50 of 660 nM. Chelerythrine chloride inhibits the Bcl-XL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from Bcl-XL. Chelerythrine chloride induces apoptosis and autophagy	protein kinase c inhibitor	PKC	Non-epigenetic	Non-epigenetic
Chidamide	9800555	Launched	Tucidinostat (Chidamide, HBI-8000, CS-055) is a low nanomolar inhibitor of HDAC1, 2, 3, and 10, the HDAC isotypes well documented to be associated with the malignant phenotype with IC50 values of 95, 160, 67, 78 nM for HDAC1, 2, 3, 10 respectively	hdac inhibitor	HDAC10 | HDAC3	Eraser	HDACi
Chidamide + Cytarabine		Preclinical	Combination: Chidamide + Cytarabine	hdac inhibitor | ribonucleotide reductase inhibitor	HDAC10 | HDAC3 | POLA1 | POLB | POLD1 | POLE	Eraser | Non-epigenetic	HDACi | Non-epigenetic
Chloramphenicol	5959	Launched	Inhibits mitochondrial gene translation and OXPHOS assembly and function	bacterial 50s ribosomal subunit inhibitor	CD55 | CYP2C19	Non-epigenetic	Non-epigenetic
Chlorprothixene	667467	Launched	Chlorprothixene is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity.	dopamine receptor antagonist	CHRM1 | CHRM2 | CHRM3 | CHRM4 | CHRM5 | DRD1 | DRD2 | DRD3 | HRH1 | HTR2A | HTR2B | HTR2C	Non-epigenetic	Non-epigenetic
CHM-1	375860	Preclinical	Inducer of apoptosis; displays potent antitumor ability in human hepatocellular carcinoma. Inhibits tubulin polymerization in vitro and in vivo. Causes cell cycle arrest at G2/M phase by activation of Cdc2 kinase activity. Induces translocation of apoptosis inducing factor(AIF) from the mitochondria to nucleus. Also exhibits vascular targeting activity through upregulation of p53 and induction of death receptor (DR5)-mediated apoptosis in HUVEC cells	tubulin polymerization inhibitor	TUBB	Non-epigenetic	Non-epigenetic
Ciclopirox	2749	Launched	Synthetic antifungal agent.	membrane integrity inhibitor	ATP1A1	Non-epigenetic	Non-epigenetic
Cilengitide	176873	Phase 3	Cilengitide (EMD 121974) is a potent integrins antagonist with IC50s of 0.61 nM (ανβ3), 8.4 nM (ανβ5) and 14.9 nM (α5β1), respectively. Cilengitide inhibits the binding of ανβ3 and ανβ5 to Vitronectin with IC50s of 4 nM and 79 nM, respectively. Cilengitide inhibits TGF-β/Smad signaling, mediates PD-L1 expression. Cilengitide also induces apoptosis, shows antiangiogenic effect in the research against glioblastoma and other cancers	integrin antagonist	ITGAV | ITGB3 | ITGB5	Non-epigenetic	Non-epigenetic
Cinacalcet	156419	Launched	Cinacalcet (AMG 073) is an orally active, allosteric agonist of Ca receptor (CaR), used for cardiovascular disease research	calcium channel activator	CASR	Non-epigenetic	Non-epigenetic
Ciril_iCDK9		Preclinical	CDK9 Inhibitor	cdk inhibitor	CDK9	Non-epigenetic	Non-epigenetic
Cisplatin	5702198	Launched	Inorganic platinum complex, which is able to inhibit DNA synthesis by conforming DNA adducts in tumor cells. Cisplatin activates ferroptosis and induces autophagy	dna alkylating agent | dna synthesis inhibitor	FASLG | SLC22A2 | TXNRD1 | TXNRD2 | XIAP	Non-epigenetic	Non-epigenetic
Cladribine	20279	Launched	Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis	adenosine deaminase inhibitor | ribonucleotide reductase inhibitor	ADA | PNP | POLA1 | POLE | POLE2 | POLE3 | POLE4 | RRM1 | RRM2 | RRM2B	Non-epigenetic	Non-epigenetic
Clarithromycin	84029	Launched	Clarithromycin has a broad spectrum of antimicrobial activity. Clarithromycin inhibits the CYP3A4-catalyzed triazolam alpha-hydroxylation with the IC50 (Ki) value of 56 (43) μM. Clarithromycin significantly inhibits the HERG potassium current.Clarithromycin affects the autophagic flux by impairing the signaling pathway linking hERG1 and PI3K	bacterial 50s ribosomal subunit inhibitor	CYP2C19 | CYP3A4 | CYP3A5 | CYP3A7	Non-epigenetic	Non-epigenetic
Clofarabine	119182	Launched	Clofarabine (Clolar) inhibits the enzymatic activities of ribonucleotide reductase (RNR) (IC50 = 65 nM) and DNA polymerase. Clofarabine induces autophagy and apoptosis	ribonucleotide reductase inhibitor	POLA1 | POLD1 | POLE | RRM1 | RRM2 | RRM2B | SLC22A8	Non-epigenetic	Non-epigenetic
CM03	137203116	Preclinical	CM03 is a trisubstituted naphthalene diimide compound previously shown to have equivalent potency to gemcitabine in the pancreatic cancer cell line MIA PaCa-2	ribonucleotide reductase inhibitor	CMPK1 | RRM1 | RRM2 | TYMS	Non-epigenetic	Non-epigenetic
Cobimetinib	16222096	Launched	Cobimetinib (GDC-0973, RG7420) is a potent, selective and oral MEK1 inhibitor with an IC50 of 4.2 nM for MEK1	mek inhibitor	MAP2K1	Non-epigenetic	Non-epigenetic
Combretastatin	9895264	Preclinical	Combretastatin is a stilbenoid phenol, originally isolated from the bark of the African bush willow tree Combretum caffrum, with vascular disrupting and antineoplastic activities. Combretastatin targets and binds to the colchicine-binding site of tubulin, thereby impairs the polymerization of tubulin dimers and prevents the formation of microtubules in the endothelial cells of tumor. As a result, this may eventually lead to a destruction of the tumor vasculature, disruption of tumor blood flow and tumor cell necrosis.	tubulin polymerization inhibitor	TUBB	Non-epigenetic	Non-epigenetic
Compound Kushen Injection		Preclinical	Traditional Chinese medicine; Compound Kushen Injection (CKI)	cell cycle inhibitor		Non-epigenetic	Non-epigenetic
Compound Kushen Injection + 5-Fluorouracil		Preclinical	Combination: CKI + 5-Fluorouracil	cell cycle inhibitor | thymidylate synthase inhibitor	CD44 | DPYD | TYMS	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Compound Kushen Injection + Doxorubicin		Preclinical	Combination: CKI + Doxorubicin	cell cycle inhibitor | topoisomerase inhibitor	TOP2A	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Compound Kushen Injection N-Mac		Preclinical	Traditional Chinese medicine; Compound Kushen Injection (CKI) w/o Mac	cell cycle inhibitor		Non-epigenetic	Non-epigenetic
Compound Kushen Injection N-MacOmtOspc		Preclinical	Traditional Chinese medicine; Compound Kushen Injection (CKI) w/o Mac Omt and Ospc	cell cycle inhibitor		Non-epigenetic	Non-epigenetic
Compound Kushen Injection N-Nme		Preclinical	Traditional Chinese medicine; Compound Kushen Injection (CKI) w/o Nme	cell cycle inhibitor		Non-epigenetic	Non-epigenetic
Compound Kushen Injection N-Omt		Preclinical	Traditional Chinese medicine; Compound Kushen Injection (CKI) w/o Omt	cell cycle inhibitor		Non-epigenetic	Non-epigenetic
Compound Kushen Injection N-OmtOspc		Preclinical	Traditional Chinese medicine; Compound Kushen Injection (CKI) w/o Omt and Ospc	cell cycle inhibitor		Non-epigenetic	Non-epigenetic
Compound Kushen Injection N-Tri		Preclinical	Traditional Chinese medicine; Compound Kushen Injection (CKI) w/o Tri	cell cycle inhibitor		Non-epigenetic	Non-epigenetic
Copanlisib	135565596	Launched	Copanlisib (BAY 80-6946) is a potent, selective and ATP-competitive pan-class I PI3K inhibitor, with IC50s of 0.5 nM, 0.7 nM, 3.7 nM and 6.4 nM for PI3Kα, PI3Kδ, PI3Kβ and PI3Kγ, respectively. Copanlisib has more than 2,000-fold selectivity against other lipid and protein kinases, except for mTOR. Copanlisib has superior antitumor activity	pi3k inhibitor	PIK3CA | PIK3CB | PIK3CD | PIK3CG	Non-epigenetic	Non-epigenetic
Cotyledon orbiculata		Preclinical	South African medicinal plant, had an anti-proliferative effect in cancer cells, mediated by apoptosis induced by alternative splicing of hnRNPA2B1 and BCL2L1	rna splicing modifier	BCL1 | BCL2 | HNRNPA2B1	Non-epigenetic	Non-epigenetic
CP-100356 monohydrochloride	71312025	Preclinical	CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM)	bcrp inhibitor | mdr1 inhibitor	BCRP | MDR1	Non-epigenetic	Non-epigenetic
CP-31398 dihydrochloride hydrate	56972205	Preclinical	CP-31398 dihydrochloride stabilizes the active conformation of p53 and promotes p53 activity in cancer cell lines with mutant or wild-type p53	p53 stabilizing agent	TP53	Non-epigenetic	Non-epigenetic
CP1203		Preclinical	CBP/EP300 Bromodomain inhibition	bromodomain inhibitor	BRD2 | BRD3 | BRD4 | BRDT	Reader	PAHi
CP724714	9874913	Phase 2	CP-724714 is a potent, selective and orally active ErbB2 (HER2) tyrosine kinase inhibitor, with an IC50 of 10 nM. CP-724714 displays a marked selectivity against EGFR kinase (IC50=6400 nM). CP-724714 potently inhibits ErbB2 receptor autophosphorylation in intact cells. Antitumor activities	egfr inhibitor | protein tyrosine kinase inhibitor	ERBB2	Non-epigenetic	Non-epigenetic
Cpd188	1652812	Preclinical	C188 is a STAT3 inhibitor that inhibits IL-6-stimulated STAT3 phosphorylation and nuclear translocation in HepG2 cells by targeting STAT3 SH2 domain peptide-binding pocket. C188, in particular, was highly active in inducing apoptosis of the breast cancer cell line MB-MDA-468 in vitro (EC50= 0.7 μM).	stat inhibitor	STAT3	Non-epigenetic	Non-epigenetic
CPI-360	73442743	Preclinical	CPI-360 is a potent, selective EZH2inhibitor with IC50 of 0.5 nM and 2.5 nM nM for wt EZH2 and Y641N EZH2, respectively.	histone lysine methyltransferase inhibitor	EZH2	Writer	HMTi
CPI-670242		Preclinical	LSD1 inhibitor	histone lysine demethylase inhibitor	KDM1A	Eraser	HDMi
CPI613	24770514	Phase 3	Devimistat (CPI-613) is a mitochondrial metabolism inhibitor. Devimistat is a lipoic acid antagonist that abrogates mitochondrial energy metabolism to induce apoptosis in various cancer cells	pyruvate dehydrogenase inhibitor	OGDH | PDHA1	Non-epigenetic	Non-epigenetic
Crenolanib	10366136	Phase 3	Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively	pdgfr tyrosine kinase receptor inhibitor	CSF1R | FLT3 | KIT | PDGFRA | PDGFRB	Non-epigenetic	Non-epigenetic
Crizotinib	11626560	Launched	Inhibitor of c-Met and ALK with IC50 of 11 nM and 24 nM, respectively.	alk tyrosine kinase receptor inhibitor	ALK | CYP2B6 | CYP3A5 | MET | MST1R | ROS1	Non-epigenetic	Non-epigenetic
Cyclocreatine	2896	Phase 1	Decreases the rate of ATP production via creatine kinase and reduces the proliferation of tumor cell lines that are characterized by high levels of creatine kinase expression	creatine kinase substrate		Non-epigenetic	Non-epigenetic
Cyclophosphamide	2907	Launched	Cyclophosphamide is a synthetic alkylating agent chemically related to the nitrogen mustards with antineoplastic activity, a immunosuppressant	dna alkylating agent	BCL2 | CYP2A6 | CYP2B6 | CYP2C18 | CYP2C19 | CYP2C8 | CYP2C9 | CYP2D6 | CYP3A4 | CYP3A5 | CYP3A7 | LGALS1	Non-epigenetic	Non-epigenetic
Cyclosporine	5284373	Launched	Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC50 of 5 nM. Cyclosporin A also inhibits CD11a/CD18 adhesion	calcineurin inhibitor	ABCB11 | CAMLG | CYP3A5 | CYP3A7 | FPR1 | PPIA | PPID | PPIF | PPP3CA | PPP3R2 | SLC10A1 | SLCO1B1 | SLCO1B3	Non-epigenetic	Non-epigenetic
Cyproterone	5284537	Launched	Cyproterone acetate is an anti-androgen (IC50=7.1 nM) and progestogen synthetic steroid. Cyproterone acetate has affinity with progesteron and with glucocorticoidal receptors	androgen receptor antagonist	ADORA1 | AR	Non-epigenetic	Non-epigenetic
Cytarabine	6253	Launched	Cytarabine is an antimetabolic agent and DNA synthesis inhibitor with IC50 of 16 nM in wild-type CCRF-CEM cells. Cytarabine induces autophagy and apoptosis	ribonucleotide reductase inhibitor	POLA1 | POLB | POLD1 | POLE	Non-epigenetic	Non-epigenetic
D2 receptor		Preclinical	3'-Fluorobenzylspiperone maleate is a very potent and selective ligand for the D2 receptor (Ki = 0.023 nM). Compared with spiperone, displays a 2.5-fold greater affinity at D2 and a 12-fold lower affinity at 5-HT2 receptors	dopamine receptor ligand	DRD2	Non-epigenetic	Non-epigenetic
Dabrafenib	44462760	Launched	Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively	raf inhibitor	BRAF | CYP2B6 | CYP2C19 | CYP2C8 | CYP3A4 | LIMK1 | NEK11 | RAF1 | SIK1	Non-epigenetic	Non-epigenetic
Dacarbazine	135398738	Launched	Dacarbazine is a nonspecific antineoplastic (antineoplastic) alkylating agent. Dacarbazine inhibits T and B lymphocyte responses with IC50 of 50 and 10 μg/mL, respectively. Dacarbazine can be used in the study of metastatic malignant melanoma	dna alkylating agent	PGD | POLA2	Non-epigenetic	Non-epigenetic
Dacinostat	6445533	Phase 1	Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research	hdac inhibitor	HDAC1 | HDAC2 | HDAC3 | HDAC4 | HDAC5 | HDAC6 | HDAC7 | HDAC8 | HDAC9	Eraser	HDACi
Dacomitinib	11511120	Launched	Dacomitinib (PF-00299804) is a specific and irreversible inhibitor of the ERBB family of kinases with IC50s of 6 nM, 45.7 nM and 73.7 nM for EGFR, ERBB2, and ERBB4, respectively	egfr inhibitor	EGFR | ERBB2 | ERBB4	Non-epigenetic	Non-epigenetic
Dactolisib	11977753	Phase 3	Dactolisib (BEZ235) is an orally active and dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2	mtor inhibitor | pi3k inhibitor	ATR | MTOR | PIK3CA | PIK3CB | PIK3CD | PIK3CG	Non-epigenetic	Non-epigenetic
Danusertib	11442891	Phase 2	Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively	aurora kinase inhibitor | growth factor receptor inhibitor	AURKA | AURKB | AURKC | BCR | FGFR1 | NTRK1 | RET | SLK	Non-epigenetic	Non-epigenetic
Darolutamide	67171867	Launched	Darolutamide (ODM-201;BAY-1841788) is a potent androgen receptor (AR) antagonist with an IC50 of 26 nM in in vitro assay	androgen receptor antagonist	AR	Non-epigenetic	Non-epigenetic
Dasatinib	3062316	Launched	Multi-targeted PTK inhibitor that targets Abl, Src and c-Kit, with IC50 of 1 nM, 0.8 nM and 79 nM, respectively	bcr-abl kinase inhibitor | ephrin inhibitor | kit inhibitor | pdgfr tyrosine kinase receptor inhibitor | src inhibitor | tyrosine kinase inhibitor	ABL1 | ABL2 | BCR | BLK | BTK | DDR1 | DDR2 | EPHA2 | FGR | FRK | FYN | HCK | KIT | LCK | LYN | PDGFRA | PDGFRB | SRC | SRMS | STAT5B | YES1	Non-epigenetic	Non-epigenetic
Daunorubicin	30323	Launched	Daunorubicin is an anthracycline antineoplastic antibiotic with therapeutic effects similar to those of doxorubicin. Daunorubicin exhibits cytotoxic activity through topoisomerase-mediated interaction with DNA, thereby inhibiting DNA replication and repair and RNA and protein synthesis.	rna synthesis inhibitor | topoisomerase inhibitor	TOP2A | TOP2B	Non-epigenetic	Non-epigenetic
DBeQ	676352	Preclinical	Selective, potent, reversible, and ATP-competitive p97 inhibitor with IC50 of 1.5μM. Induces executioner caspases (caspase-3 and caspase-7) rapidly. Blocks the degradation of endoplasmic reticulum-associated degradation (ERAD) reporters; also blocks autophagosome maturation and promotes accumulation of LC3-II	atpase inhibitor	CASP3	Non-epigenetic	Non-epigenetic
dBET6	121427831	Preclinical	Highly potent, selective and cell-permeable degrader of BET based on PROTAC, with an IC50 of 14 nM, and has antitumor activity.	protac	BRD2 | BRD3 | BRD4 | BRDT	Reader	PAHi
DBK-1154		Preclinical	SMAP-2 (DT-1154) (DBK-1154?) is an orally active protein phosphatase 2A (PP2A) activator, with anti-cancer activity.	androgen receptor modulator	AR	Non-epigenetic	Non-epigenetic
Deazaneplanocin A	11615884	Preclinical	Potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor.	histone lysine methyltransferase inhibitor	AHCY | EZH2	Writer	HMTi
Decitabine	451668	Launched	Deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis	dna methyltransferase inhibitor	DNMT1 | DNMT3A	Writer	DNMTi
Decitabine + BSJ-116		Preclinical	Deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis and CDK12 degrader	dna methyltransferase inhibitor | protac	CDK12 | DNMT1 | DNMT3A	Writer | Non-epigenetic	DNMTi | Non-epigenetic
Decitabine + dBET6		Preclinical	Deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis and dBET6: Highly potent, selective and cell-permeable degrader of BET based on PROTAC, with an IC50 of 14 nM, and has antitumor activity.	dna methyltransferase inhibitor | protac	BRD2 | BRD3 | BRD4 | BRDT | DNMT1 | DNMT3A	Reader | Writer	DNMTi | PAHi
Decitabine + Deazaneplanocin A		Preclinical	Combination: (Decitabine) Deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. And (DZNEP) Potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A is a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor.	dna methyltransferase inhibitor | histone lysine methyltransferase inhibitor	AHCY | DNMT1 | DNMT3A | EZH2	Writer | Writer	DNMTi | HMTi
Decitabine + Depsipeptide		Preclinical	Combination: (Decitabine) Deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. and (Depsipeptide) Histone deacetylase (HDAC) inhibitor with anti-tumor activities	dna methyltransferase inhibitor | hdac inhibitor	CYP2B6 | CYP2C19 | CYP3A5 | DNMT1 | DNMT3A | HDAC1 | HDAC2 | HDAC3 | HDAC4 | HDAC5 | HDAC6 | HDAC7 | HDAC8 | HDAC9	Eraser | Writer	DNMTi | HDACi
Decitabine + GSK343		Preclinical	Combination: (Decitabine) Deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. and (GSK343) Histone Lysine Methyltransferase EZH1/2 inhibitor	dna methyltransferase inhibitor | histone lysine methyltransferase inhibitor	DNMT1 | DNMT3A | EZH2	Writer | Writer	DNMTi | HMTi
Decitabine + HH1		Preclinical	Combination: (Decitabine) Deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. and (HH1) (MC180295) is a novel potent and selective CDK9 inhibitor with an IC50 of 5 nM and is at least 22-fold more selective for CDK9 over other CDKs	cdk inhibitor | dna methyltransferase inhibitor	CDK9 | DNMT1 | DNMT3A	Writer | Non-epigenetic	DNMTi | Non-epigenetic
Decitabine + Proscillaridin A		Preclinical	Combination: (Decitabine) Deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. And (Proscillaridin A) Potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively.	dna methyltransferase inhibitor | topoisomerase inhibitor	DNMT1 | DNMT3A | TOP2A | TOP2B	Writer | Non-epigenetic	DNMTi | Non-epigenetic
Decitabine + Retinoic Acid		Preclinical	Combination: (Decitabine) Deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. And retinoic acid	dna methyltransferase inhibitor | retinoic acid signaling	DNMT1 | DNMT3A | ALDH1A1 | ALDH1A2 | GPRC5A | NR0B1 | NR2C2 | PPARD | RARA | RARB | RARG | RARRES1 | RORB | RORC | RXRB | RXRG	Writer | Non-epigenetic	DNMTi | Non-epigenetic
Decitabine + S2101		Preclinical	Combination: (Decitabine) Deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. And (S2101) Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s.	dna methyltransferase inhibitor | histone lysine demethylase inhibitor	DNMT1 | DNMT3A | EZH2	Eraser | Writer	DNMTi | HDMi | HMTi
Decitabine + siCHD4		Preclinical	Combination: (Decitabine) Deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. And (siCHD4)	dna methyltransferase inhibitor | topoisomerase inhibitor	DNMT1 | DNMT3A | TOP2A	Writer | Non-epigenetic	DNMTi | Non-epigenetic
Decitabine + TCR105		Preclinical	Combination: (Decitabine) Deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. And (TCR105)	chimeric antibody | dna methyltransferase inhibitor	CD105 | DNMT1 | DNMT3A	Writer | Non-epigenetic	DNMTi | Non-epigenetic
Decitabine + UNC0638		Preclinical	Combination: (Decitabine) Deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis. And (UNC0638) selectively inhibits G9a and GLP histone methyltransferase activity with IC50s of less than 15 nM and 19 nM, respectively. UNC0638 has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities	dna methyltransferase inhibitor | histone lysine methyltransferase inhibitor	DNMT1 | DNMT3A | EHMT1 | EHMT2	Writer | Writer	DNMTi | HMTi
Depsipeptide	5352062	Launched	Histone deacetylase (HDAC) inhibitor with anti-tumor activities	hdac inhibitor	CYP2B6 | CYP2C19 | CYP3A5 | HDAC1 | HDAC2 | HDAC3 | HDAC4 | HDAC5 | HDAC6 | HDAC7 | HDAC8 | HDAC9	Eraser	HDACi
Dexamethasone	5743	Launched	Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes.	glucocorticoid receptor agonist	ANXA1 | CYP3A4 | CYP3A5 | NOS2 | NR0B1 | NR3C1 | NR3C2	Non-epigenetic	Non-epigenetic
Dexamethasone + IL7		Preclinical	Combination: (Dexamethasone) Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. And (IL7)	glucocorticoid receptor agonist | interferon receptor agonist	ANXA1 | CYP3A4 | CYP3A5 | IL7 | NOS2 | NR0B1 | NR3C1 | NR3C2	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
DHT	10635	Preclinical	Dihydrotestosterone stimulation	dihydrotestosterone stimulation	AR	Non-epigenetic	Non-epigenetic
DHT + siCDK7		Preclinical	Combination: Dihydrotestosterone stimulation + CDK7 knockdown	cdk inhibitor | dihydrotestosterone stimulation	AR | CDK7	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
DHT + siMED1		Preclinical	Combination: Dihydrotestosterone stimulation + MED1 knockdown	dihydrotestosterone stimulation | med1 inhibitor	AR, MED1	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
DHT + siNT		Preclinical	Combination: Dihydrotestosterone stimulation + NT knockdown	dihydrotestosterone stimulation | nt inhibitor	AR | NT	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
DHT + THZ1		Preclinical	Combination: Dihydrotestosterone stimulation + THZ1	cdk inhibitor | dihydrotestosterone stimulation	AR | CDK7	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Dihydroouabain	6852401	Preclinical	Dihydroouabain, a derivative of ouabain in which the lactone ring is saturated, is about 50-fold less potent than ouabain as an inhibitor of Na+, K+-pump and does not stimulate the pump at low doses	atpase inhibitor	ATP1A1 | ATP1A2 | ATP1A3 | ATP1A4 | ATP1B1 | ATP1B2 | ATP1B3 | ATP1B4 | FXYD2	Non-epigenetic	Non-epigenetic
Dinaciclib	46926350	Phase 3	Inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM, respectively. It also blocks thymidine (dThd) DNA incorporation. Phase 3	cdk inhibitor	CCNT1 | CDK1 | CDK2 | CDK5 | CDK9	Non-epigenetic	Non-epigenetic
Diphenyleneiodonium chloride	2733504	Preclinical	Diphenyleneiodonium chloride is a NADPH oxidase (NOX) inhibitor and also functions as a TRPA1 activator with an EC50 of 1 to 3 μM. Diphenyleneiodonium chloride selectively inhibits intracellular reactive oxygen species.	nitric oxide synthase inhibitor	ALDH1A2 | ALDH2 | ALDH5A1 | ALDH7A1 | NOS2 | NOS3 | NOX3 | XDH	Non-epigenetic	Non-epigenetic
DIPPA hydrochloride	45073425	Preclinical	DIPPA (hydrochloride) is an irreversible, long-lasting, selective and high affinity κ-opioid receptor antagonist. DIPPA (hydrochloride) can be used for the research of anxiety and antidepressant	kappa opiod receptor antagonist	OPRK1	Non-epigenetic	Non-epigenetic
Disulfiram	3117	Launched	Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells. Disulfiram, a copper ion carrier, with Cu2+ increases intracellular ROS levels and induces cuproptosis	aldehyde dehydrogenase inhibitor | dna methyltransferase inhibitor | trpv agonist	ALDH1A2 | ALDH2 | ALDH5A1 | ALDH7A1 | CYP2E1 | DBH | DNMT1 | TRPA1	Writer | Non-epigenetic	DNMTi | Non-epigenetic
DMNQ	3136	Preclinical	DMNQ is a redox cycling agent. DMNQ produces hydrogen peroxide in cells in a concentration-dependent manner. DMNQ can induce the increase of ROS production	redox cycling agent	ROS	Non-epigenetic	Non-epigenetic
DMSO	679	Preclinical	Dimethyl sulfoxide (DMSO) is an aprotic solvent that dissolves both polar and nonpolar compounds. Dimethyl sulfoxide has anti-freezing and bacteriostatic properties.	control vehicle		Non-epigenetic	Non-epigenetic
Docetaxel	148124	Launched	Microtubule disassembly inhibitor with IC50 in a range of 0.31100 nM.	tubulin polymerization inhibitor	BCL2 | MAP2 | MAP4 | MAPT | NR1I2 | TUBA1A | TUBA1B | TUBA1C | TUBA3C | TUBA3D | TUBA3E | TUBA4A | TUBB | TUBB1 | TUBB2A | TUBB2B | TUBB3 | TUBB4A | TUBB4B | TUBB6 | TUBB8	Non-epigenetic	Non-epigenetic
Dorsomorphin dihydrochloride	49761481	Preclinical	Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride can reverse autophagy activation and anti-inflammatory effect of Urolithin A (HY-100599)	ampk inhibitor	ACVR1 | BMPR1A | BMPR1B | EPHA2 | FKBP1A | FLT1 | FLT3 | KDR | LCK | MKNK1 | PRKAA1 | RPS6KA1 | SRC	Non-epigenetic	Non-epigenetic
Dovitinib	135398510	Phase 3	Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity	egfr inhibitor | fgfr inhibitor | flt3 inhibitor | pdgfr tyrosine kinase receptor inhibitor | vegfr inhibitor	CSF1R | EGFR | FGFR1 | FGFR2 | FGFR3 | FLT1 | FLT3 | FLT4 | INSR | KDR | KIT | PDGFRA | PDGFRB	Non-epigenetic	Non-epigenetic
Doxorobicin + Cytarabine		Preclinical	Combination: (Doxorubicin) Antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis. And (Cytarabine) a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC50 of 16 nM. Cytarabine has antiviral effects against HSV	ribonucleotide reductase inhibitor | topoisomerase inhibitor	DNMT1 | DNMT3A | POLA1 | POLB | POLD1 | POLE | TOP2A	Writer | Non-epigenetic	DNMTi | Non-epigenetic
Doxorubicin	31703	Preclinical	Antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis.	dna polymerase inhibitor | topoisomerase inhibitor	TOP2A	Non-epigenetic	Non-epigenetic
Doxorubicin + Cytarabine + Decitabine		Preclinical	Combination: (Doxorubicin) Antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis. And (Cytarabine) a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC50 of 16 nM. Cytarabine has antiviral effects against HSV. And (Decitabine) Deoxycytidine analogue antimetabolite and a DNA methyltransferase inhibitor. Decitabine incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine induces cell G2/M arrest and cell apoptosis	dna methyltransferase inhibitor | dna polymerase inhibitor | ribonucleotide reductase inhibitor | topoisomerase inhibitor	DNMT1 | DNMT3A | POLA1 | POLB | POLD1 | POLE | TOP2A	Writer | Non-epigenetic	DNMTi | Non-epigenetic
Doxorubicin + MDL72527		Preclinical	Combination: Doxorubicin + MDL72527	dna polymerase inhibitor | spermine oxidase smo inhibitor | topoisomerase inhibitor	SMO | TOP2A	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Doxorubicin + Prexasertib + Gemcitabine		Preclinical	Combination: Doxorubicin + Prexasertib + Gemcitabine	chk inhibitor | dna polymerase inhibitor | ribonucleotide reductase inhibitor | topoisomerase inhibitor	CHEK1 | CMPK1 | RRM1 | RRM2 | TOP2A | TYMS	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Doxycycline	54671203	Launched	Doxycycline, an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.	bacterial 30s ribosomal subunit inhibitor | metalloproteinase inhibitor	MMP1 | MMP8	Non-epigenetic	Non-epigenetic
Doxycycline induced sh2025		N/A	shRNA targeting BRM	short hairpin rna	SMARCA2 | SMARCA4	Remodeler	Non-epigenetic
Doxycycline induced sh5537		N/A	shRNA targeting BRM	short hairpin rna	SMARCA2 | SMARCA4	Remodeler	Non-epigenetic
DU145-Docetaxel-resistant		Preclinical		N/A		Non-epigenetic	Non-epigenetic
Duvelisib	50905713	Launched	Duvelisib (IPI-145) is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively	pi3k inhibitor	PIK3CA | PIK3CB | PIK3CD | PIK3CG	Non-epigenetic	Non-epigenetic
E64FC65	137796284	Preclinical	Protein disulfide isomerase inhibitor	calpain inhibitor | cysteine protease inhibitor	CTSS	Non-epigenetic	Non-epigenetic
E64FC65 + Panobinostat		Preclinical	Combination: Protein disulfide isomerase inhibitor and Panobinostat	calpain inhibitor | cysteine protease inhibitor | hdac inhibitor	CTSS | HDAC1 | HDAC2 | HDAC3 | HDAC4 | HDAC6 | HDAC7 | HDAC8 | HDAC9	Eraser | Non-epigenetic	HDACi | Non-epigenetic
E64FC65 + Panobinostat + shRNA		Preclinical	Combination: Protein disulfide isomerase inhibitor and ATF3 knockdown	calpain inhibitor | cysteine protease inhibitor | hdac inhibitor	CTSS | HDAC1 | HDAC2 | HDAC3 | HDAC4 | HDAC6 | HDAC7 | HDAC8 | HDAC9	Eraser | Non-epigenetic	HDACi | Non-epigenetic
E64FC65 + Panobinostat + siRNA		Preclinical	Combination: Protein disulfide isomerase inhibitor and ATF3 knockout	calpain inhibitor | cysteine protease inhibitor | hdac inhibitor	CTSS | HDAC1 | HDAC2 | HDAC3 | HDAC4 | HDAC6 | HDAC7 | HDAC8 | HDAC9	Eraser | Non-epigenetic	HDACi | Non-epigenetic
E7107	16202132	Preclinical	E7107 blocks spliceosome assembly by preventing tight binding of U2 snRNP to pre-mRNA	rna splicing inhibitor	U2	Non-epigenetic	Non-epigenetic
EC-8042		Launched	Mithramycin analog (SP1-inhibitor )	rna synthesis inhibitor	SP1	Non-epigenetic	Non-epigenetic
Elesclomol	300471	Phase 3	Elesclomol (STA-4783) is a potent copper ionophore and promotes copper-dependent cell death (cuproptosis). Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand. Elesclomol inhibits FDX1-mediated Fe-S cluster biosynthesis. Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research	oxidative stress inducer	HSPA1A | TOP2A	Non-epigenetic	Non-epigenetic
Ellipticine	3213	Preclinical	Ellipticine (NSC 71795) is a potent antineoplastic agent; inhibits DNA topoisomerase II activities	topoisomerase inhibitor	TOP2A	Non-epigenetic	Non-epigenetic
Elraglusib	44582816	Phase 2	9-ING-41 (Elraglusib) is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic agents	gsk3b inhibitor	GSK3B | MARK2	Non-epigenetic	Non-epigenetic
Emetine dihydrochloride hydrate (Emetine)	10219	Phase 2	Emetine dihydrochloride hydrate is a hydrate that is the monohydrate of the dihydrochloride salt of emetine. It has a role as an antimalarial, an antineoplastic agent, an antiprotozoal drug, an antiviral agent, an autophagy inhibitor, an emetic, a protein synthesis inhibitor and an anticoronaviral agent	protein synthesis inhibitor	RPS2	Non-epigenetic	Non-epigenetic
Enasidenib	89683805	Launched	Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively.	isocitrate dehydrogenase inhibitor	IDH1	Non-epigenetic	Non-epigenetic
Eniluracil	43157	Phase 3	Eniluracil (5-Ethynyluracil) is an orally active dihydropyrimidine dehydrogenase (DPD) inhibitor. Eniluracil irreversibly inhibits DPD, increases the oral bioavailability of 5-fluorouracil to 100%, and facilitates the uniform absorption and toxicity of 5-fluorouracil. Eniluracil can be used in cancer research of combination with fluoropyrimidines (including 5-fluorouracil). Eniluracil is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups	dihydropyrimidine dehydrogenase inhibitor	AOX1 | DPYD | XDH	Non-epigenetic	Non-epigenetic
ENMD2076	16041424	Phase 2	ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively	aurora kinase inhibitor | flt3 inhibitor | vegfr inhibitor	AURKA | CSF1R | EPHA1 | FGFR1 | FGFR2 | FGFR3 | FLT3 | FLT4 | KDR | KIT | PDGFRA | PTK2 | SRC	Non-epigenetic	Non-epigenetic
Entinostat	4261	Phase 3	Inhibits HDAC1 and HDAC3 with IC50 of 0.51μM and 1.7μM. Phase 1/2	hdac inhibitor	HDAC1 | HDAC2 | HDAC3 | HDAC9	Eraser	HDACi
Entospletinib	59473233	Phase 2	Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with an IC50 of 7.7 nM	syk inhibitor	SYK	Non-epigenetic	Non-epigenetic
Enzalutamide	15951529	Launched	Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator	androgen receptor antagonist	AR | CYP2C19 | CYP2C8 | CYP3A4	Non-epigenetic	Non-epigenetic
Enzastaurin	176167	Phase 3	Enzastaurin (LY317615) is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε	pkc inhibitor	AKT1 | GSK3B | PRKCA | PRKCB | PRKCD | PRKCG	Non-epigenetic	Non-epigenetic
Epigallocatechin gallate	65064	Phase 2/Phase 3	(-)-Epigallocatechin (Epigallocatechin) is the most abundant flavonoid in green tea, can bind to unfolded native polypeptides and prevent conversion to amyloid fibrils	bacterial dna gyrase inhibitor	APP | CYP19A1 | DYRK1A | ELANE | ENOX2 | EP300 | FASN | IDO1 | KAT2B | KDR | MMP14 | MMP2 | PREP | SLC5A1	Writer	HATi
Epirubicin	41867	Launched	Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity	topoisomerase inhibitor	CHD1 | TOP2A	Remodeler	Non-epigenetic
Epothilone B	448013	Phase 3	Epothilone B is a microtubule stabilizer with a Ki of 0.71μM. It acts by binding to the αβ-tubulin heterodimer subunit which causes decreasing of αβ-tubulin dissociation	microtubule stabilizing agent | tubulin polymerization inhibitor	TUBB	Non-epigenetic	Non-epigenetic
Epothilone D	447865	Phase 2	Epothilone D (KOS 862) is a potent microtubule stabilizer	microtubule stabilizing agent | tubulin polymerization inhibitor	TUBB	Non-epigenetic	Non-epigenetic
EPZ-5676	57345410	Phase 1	Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM	histone lysine methyltransferase inhibitor	DOT1L	Writer	HMTi
EPZ004777	56962336	Preclinical	EPZ004777 is a potent, selective DOT1L inhibitor with IC50 of 0.4 nM in a cell-free assay and demonstrates >1,200-fold selectivity for DOT1L over all other tested PMTs. EPZ004777 induces apoptosis.	histone lysine methyltransferase inhibitor	DOT1L	Writer	HMTi
ER 27319 maleate	56972172	Preclinical	ER-27319 (maleate), an acridone derivative, is a potent and selective SKY inhibitor, and inhibits the tyrosine phosphorylation of SYK and its activity. ER-27319 (maleate) inhibits the release of antigen-induced allergic mediators from human and rat mast cells with an IC50 of 10 μM and can be used for study in allergic diseases	mediator release inhibitor | syk inhibitor	SYK	Non-epigenetic	Non-epigenetic
Erastin	11214940	Preclinical	Erastin is a ferroptosis activator by acting on mitochondrial VDAC, exhibiting selectivity for tumor cells bearing oncogenic RAS.	ion channel antagonist	VDAC2	Non-epigenetic	Non-epigenetic
Erlotinib	176870	Launched	EGFR tyrosine kinase inhibitor, with an IC50 of 2 nM for human EGFR. Erlotinib reduces EGFR autophosphorylation in intact tumor cells with an IC50 of 20 nM. Erlotinib is used for the treatment of non-small cell lung cancer.	egfr inhibitor	EGFR | NR1I2	Non-epigenetic	Non-epigenetic
Estramustine	259331	Launched	Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts	dna alkylating agent	ESR1 | ESR2 | MAP1A | MAP2	Non-epigenetic	Non-epigenetic
Estrogen	448537	Withdrawn	Estrogen	estrogen receptor agonist	ESR1 | ESR2 | ESRRB | ESRRG	Non-epigenetic	Non-epigenetic
Etonitazenyl isothiocyanate	128795	Preclinical	Etonitazenyl isothiocyanate is a μ-opioid selective irreversible affinity label	u-opioid receptor agonist	MOR	Non-epigenetic	Non-epigenetic
Etoposide	36462	Launched	Inhibits topoisomerase II, thus stopping DNA replication. Etoposide induces cell cycle arrest, apoptosis and autophagy	topoisomerase inhibitor	CYP2E1 | CYP3A5 | TOP2A | TOP2B	Non-epigenetic	Non-epigenetic
Etoposide + Rapamycin		Preclinical	Combination: Etoposide + Rapamycin	mtor inhibitor | topoisomerase inhibitor	CYP2E1 | CYP3A5 | MTOR | TOP2A | TOP2B	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Everolimus	6442177	Launched	mTOR and FKBP12 inhibitor with IC50 of 1.6-2.4 nM.	mtor inhibitor	CYP3A5 | FKBP1A | MTOR	Non-epigenetic	Non-epigenetic
EX00101218	25104564	Preclinical	LDC000067 (EX00101218) is a highly selective CDK9 inhibitor with IC50 of 44 nM, 55/125/210/ >227/ >227-fold selectivity over CDK2/1/4/6/7.	cdk inhibitor	CDK9	Non-epigenetic	Non-epigenetic
Exemestane	60198	Launched	Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research	aromatase inhibitor	CYP19A1	Non-epigenetic	Non-epigenetic
Ezatiostat	5310939	Phase 2	Ezatiostat (TER199 free base; TLK199) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat leads to JNK activation by inhibiting GSTP1. Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat has the potential for myelodysplastic syndrome (MDS) treatment	glutathione transferase inhibitor	GSTP1	Non-epigenetic	Non-epigenetic
FB23	138393314	Preclinical	FB23 is a potent and selective FTO demethylase inhibitor with an IC50 of 60 nM. FB23 directly binds to FTO and selectively inhibits FTO's mRNA N6-methyladenosine (m6A) demethylase activity.	fto demethylase inhibitor	FTO	Eraser	HDMi
FB23-2	138454779	Preclinical	FB23-2 is a potent and selective inhibitor of mRNA N6-methyladenosine (m6A) demethylase FTO, with an IC50 of 2.6 μM. FB23-2 has anti-proliferation activity. FB23-2 can be used for the research of acute myeloid leukemia (AML).	fto demethylase inhibitor	FTO	Eraser	HDMi
FBS + L-Glucose		Preclinical	Combination: FBS + L-Glucose	growth supplement		Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Fedratinib	16722836	Launched	Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research	flt3 inhibitor | jak inhibitor	BRD4 | FLT3 | JAK1 | JAK2 | JAK3 | RET | TYK2	Reader	PAHi
Finasteride	57363	Launched	Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia	5 alpha reductase inhibitor	AKR1D1 | AR | SRD5A1 | SRD5A2	Non-epigenetic	Non-epigenetic
Fingolimod	107970	Launched	Inhibitor of mutubule motor protein HSET with IC50 of 75μM, significant selectivity over KSP.	immunosuppressant | sphingosine 1-phosphate receptor agonist	CYP2E1 | CYP4F2 | S1PR1 | S1PR3 | S1PR4 | S1PR5 | SPHK1	Non-epigenetic	Non-epigenetic
FIT	84008	Preclinical	specific reagent for irreversible inactivation of delta opiate receptors in rat brain membranes	opioid receptor agonist	OPRD1	Non-epigenetic	Non-epigenetic
FK866	6914657	Phase 2	Inhibits nicotinamide phosphoribosyl transferase (NMPRTase) with IC50 of 0.09 nM in a cell-free assay. Phase 1/2	niacinamide phosphoribosyltransferase inhibitor	NAMPT | PARP1	Non-epigenetic	Non-epigenetic
Flavopiridol	5287969	Phase 2	Competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of 40 nM. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridolis initially found to inhibit EGFR and PKA. Phase 1/2	cdk inhibitor	BCL2 | BIRC5 | CCNT1 | CDK1 | CDK2 | CDK4 | CDK5 | CDK6 | CDK7 | CDK8 | CDK9 | EGFR | MCL1 | PYGM | XIAP	Non-epigenetic	Non-epigenetic
Floxuridine	5790	Launched	Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis. Floxuridine has antiviral effects against HSV and CMV	dna synthesis inhibitor	TYMS	Non-epigenetic	Non-epigenetic
Fludarabine	657237	Launched	Fludarabine is a STAT1 activation inhibitor which causes a specific depletion of STAT1 protein (and mRNA) but not of other STATs. Also a DNA synthesis inhibitor in vascular smooth muscle cells. Fludarabine induces apoptosis.	ribonucleotide reductase inhibitor	ADA | DCK | POLA1 | RRM1 | RRM2	Non-epigenetic	Non-epigenetic
Fluvastatin	446155	Launched	Inhibits HMG-CoA reductase activity with IC50 of 8 nM	hmgcr inhibitor	CYP2C8 | HMGCR	Non-epigenetic	Non-epigenetic
Foretinib	42642645	Phase 2	ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM. Less potent against Ron, Flt-1/3/4, Kit, PDGFRα/βand Tie-2, and little activity to FGFR1 and EGFR. Phase 2	vegfr inhibitor	AXL | FLT1 | FLT3 | FLT4 | KDR | KIT | MET | MST1R | TEK	Non-epigenetic	Non-epigenetic
Fotemustine	104799	Launched	Fotemustine is a nitrosourea alkylating agent used in the treatment of metastatic melanoma.	thioredoxin inhibitor		Non-epigenetic	Non-epigenetic
Fulvestrant	104741	Launched	Fulvestrant (ICI 182780) is a pure antiestrogen and a potent estrogen receptor (ER) antagonist with an IC50 of 9.4 nM. Fulvestrant is also a GPR30 agonist. Fulvestrant effectively inhibits the growth of ER-positive MCF-7 cells with an IC50 of 0.29 nM. Fulvestrant also induces autophagy and has antitumor efficacy.	estrogen receptor antagonist	EPHX2 | ESR1 | ESR2 | GPER1	Non-epigenetic	Non-epigenetic
Galeterone	11188409	Phase 3	Galeterone (TOK-001) is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC)	androgen receptor modulator	AR | CYP17A1	Non-epigenetic	Non-epigenetic
Galunisertib	10090485	Phase 2/Phase 3	Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.	tgf beta receptor inhibitor	TGFBR1	Non-epigenetic	Non-epigenetic
Ganetespib	135564985	Phase 3	Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3	hsp inhibitor	HSP90AA1 | WT1	Non-epigenetic	Non-epigenetic
GB1874	24242759	Preclinical	GB1874 is an inhibitor of the Wnt pathway targeting β-catenin-TCF4 protein-protein interaction (PPI), affecting proliferation and stemness in Wnt-dependent colorectal cancer (CRC) cells and inhibiting the growth of HCT116 tumour xenografts in vivo.	wnt pathway inhibitor	TCF4 | WNT	Non-epigenetic	Non-epigenetic
GB6853		Preclinical	Inhibition of Wnt signaling by disruption of the β-catenin (β-cat)-TCF4 protein-protein interaction (PPI) complex (?)	wnt pathway inhibitor	TCF4 | WNT	Non-epigenetic	Non-epigenetic
GB8679		Preclinical	Inhibition of Wnt signaling by disruption of the β-catenin (β-cat)-TCF4 protein-protein interaction (PPI) complex (?)	wnt pathway inhibitor	TCF4 | WNT	Non-epigenetic	Non-epigenetic
GBM8401-Temozolomide-resistant		N/A	Temozolomide-resistant cell line	N/A		Non-epigenetic	Non-epigenetic
GDC0068	24788740	Phase 3	Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models.	akt inhibitor	AKT1 | AKT2 | AKT3 | CYP3A5 | PRKG1	Non-epigenetic	Non-epigenetic
Gedatolisib	44516953	Phase 2	Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2	mtor inhibitor | pi3k inhibitor	MTOR | PIK3CA | PIK3CG	Non-epigenetic	Non-epigenetic
Gefitinib	123631	Launched	Gefitinib (ZD1839) is a potent, selective and orally active EGFR tyrosine kinase inhibitor with an IC50 of 33 nM. Gefitinib selectively inhibits EGF-stimulated tumor cell growth (IC50 of 54 nM) and that blocks EGF-stimulated EGFR autophosphorylation in tumor cells. Gefitinib also induces autophagy and cell apoptosis, which can be used for cancer related research, such as Lung cancer and breast cancer	egfr inhibitor	CYP2C19 | EGFR	Non-epigenetic	Non-epigenetic
Gemcitabine	60750	Launched	Deoxycytidine analogue, used as chemotherapy. Phase 3	ribonucleotide reductase inhibitor	CMPK1 | RRM1 | RRM2 | TYMS	Non-epigenetic	Non-epigenetic
Gemcitabine + Torin1		Launched | Preclinical	Combination: Gemcitabine + Torin1	mtor inhibitor | ribonucleotide reductase inhibitor	CMPK1 | MTOR | PIK3CA | RRM1 | RRM2 | TYMS	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Genistein	5280961	Phase 2/Phase 3	Genistein (NPI 031L), a phytoestrogen found in soy products, is a highly specific inhibitor of protein tyrosine kinase (PTK) which blocks the mitogenic effect mediated by EGF on NIH-3T3 cells with IC50 of 12μM or by insulin with IC50 of 19 μM	tyrosine kinase inhibitor	CFTR | EGFR | ESR1 | ESR2 | ESRRA | ESRRB | ESRRG | NCOA1 | NCOA2 | PPARG | PTK2B | TOP2A | TRPC5	Non-epigenetic	Non-epigenetic
Genistein + Gemcitabine		Phase 2/Phase 3 | Launched	Combination: Genistein + Gemcitabine	ribonucleotide reductase inhibitor | tyrosine kinase inhibitor	CFTR | CMPK1 | EGFR | ESR1 | ESR2 | ESRRA | ESRRB | ESRRG | NCOA1 | NCOA2 | PPARG | PTK2B | RRM1 | RRM2 | TOP2A | TRPC5 | TYMS	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
GFPi		N/A	GFP inhibitor	N/A		Non-epigenetic	Non-epigenetic
Gilteritinib	49803313	Launched	Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively	flt3 inhibitor	FLT3	Non-epigenetic	Non-epigenetic
Givinostat	9804992	Phase 3	Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively	hdac inhibitor	HDAC1 | HDAC2 | HDAC3 | HDAC4 | HDAC5 | HDAC6 | HDAC7 | HDAC8 | HDAC9 | IL1B | IL1R2 | IL6R | TNF	Eraser	HDACi
Glasdegib	25166913	Launched	Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM	hedgehog pathway inhibitor	DHH | IHH | SMO	Non-epigenetic	Non-epigenetic
GNF2	5311510	Preclinical	GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .	bcr-abl kinase inhibitor	ABL1 | BCR	Non-epigenetic	Non-epigenetic
Gossypol	3503	Phase 2	R-(-)enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32μM, 0.48μM and 0.18μM in cell-free assays; does not inhibit BIR3 domain and BID. Phase 2.	bcl inhibitor | mcl1 inhibitor	BCL2 | BCL2L1 | BCL2L2 | CTGF | EGF | MCL1	Non-epigenetic	Non-epigenetic
GR 127935 hydrochloride	11497466	Preclinical	GR127935 hydrochloride is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 hydrochloride can be used in neurological disease research.	5-ht1b receptor antagonist | 5-ht1d receptor antagonist	5-HT1B | 5-HT1D	Non-epigenetic	Non-epigenetic
GSK-126	68210102	Phase 1	GSK126 (GSK2816126A) is a potent, highly selective inhibitor of EZH2 methyltransferase with an IC50 of 9.9 nM.	histone lysine methyltransferase inhibitor	EZH2	Writer	HMTi
GSK-LSD1	71522234	Preclinical	LSD1 inhibitor	histone lysine demethylase inhibitor	KDM1A	Eraser	HDMi
GSK2879552	66571643	Phase 1/Phase 2	Lysine-specific histone demethylase 1 (LSD) inhibitor	histone lysine demethylase inhibitor	KDM1A	Eraser	HDMi
GSK3203591	117072552	Preclinical	Type I Protein Arginine Methyltransferases (PRMTs)	protein arginine n-methyltransferase inhibitor	PRMT1 | PRMT3 | PRMT5 | PRMT6	Writer	HMTi
GSK3203591 + GSK3368712		Preclinical	Combination: GSK3203591 + GSK3368712	protein arginine n-methyltransferase inhibitor	PRMT1 | PRMT3 | PRMT5 | PRMT6	Writer | Writer	HMTi | HMTi
GSK3368712	90462880	Preclinical	Type I Protein Arginine Methyltransferases (PRMTs)	protein arginine n-methyltransferase inhibitor	PRMT1 | PRMT3 | PRMT5 | PRMT6	Writer	HMTi
GSK343	71268957	Preclinical	Histone Lysine Methyltransferase EZH1/2 inhibitor	histone lysine methyltransferase inhibitor	EZH1 | EZH2	Writer	HMTi
GSK461364	15983966	Phase 1	Inhibits purified Plk1 with Ki of 2.2 nM. It is more than 1000-fold selective against Plk2/3.Phase 1.	plk inhibitor	PLK1	Non-epigenetic	Non-epigenetic
GSK591	117072552	Preclinical	GSK591 (EPZ015866) is a potent and selective inhibitor of protein methyltransferase 5 (PRMT5) with an IC50 of 4 nM.	protein arginine n-methyltransferase inhibitor	PRMT5	Writer	HMTi
GSK690693	16725726	Phase 1	GSK-690693 is an ATP-competitive pan-Akt inhibitor with IC50s of 2 nM, 13 nM, 9 nM for Akt1, Akt2 and Akt3, respectively. GSK-690693 is also an AMPK inhibitor, affects Unc-51-like autophagy activating kinase 1 (ULK1) activity and robustly inhibits STING-dependent IRF3 activation	akt inhibitor	AKT1 | AKT2 | AKT3 | PAK4 | PAK6 | PAK7 | PRKCQ | PRKG1 | PRKX	Non-epigenetic	Non-epigenetic
GW-405833	9911463	Preclinical	CB2 receptor partial agonist (EC50= 0.65 nM; maximum inhibition = 44.6%). Binds with high affinity to both human and rat CB2 receptors and displays 1200-fold selectivity over CB1 (Ki values are 3.92 and 4772 nM for human recombinant CB2 and CB1 receptors respectively). Produces potent antihyperalgesic effects in several rodent models of pain	cannabinoid receptor agonist	CNR2	Non-epigenetic	Non-epigenetic
GYY4137	46937261	Preclinical	GYY4137 is a slow releasing H2S donor with vasodilator and antihypertensive activity. GYY4137 also exhibits anti-inflammatory and anticancer activity.	cytokine production inhibitor | hydrogen sulfide donor	IL-1B | IL-6	Non-epigenetic	Non-epigenetic
GYY4137 + LPS		Preclinical	Combination: (GYY4137) a slow releasing H2S donor with vasodilator and antihypertensive activity. GYY4137 also exhibits anti-inflammatory and anticancer activity. And (LPS) Lipopolysaccharides (LPS) is an endotoxin derived from the outer leaflet of the outer membrane of Gram-negative bacteria. Lipopolysaccharides consists of an antigen O-specific chain, a core oligosaccharide and lipid A. Lipopolysaccharides is a highly immunogenic antigen which can enhance immune responses. This product is derived from Escherichia coli O55:B5.	hydrogen sulfide donor | inflamation inducer	IL-1B | IL-6	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Halicin	11837140	Preclinical	Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt kinase	jnk inhibitor	MAPK8	Non-epigenetic	Non-epigenetic
Halofuginone	400772	Launched	Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.	collagenase inhibitor	COL1A1 | MMP2	Non-epigenetic	Non-epigenetic
HEAT hydrochloride	6917680	Preclinical	HEAT hydrochloride is a very selective α1-adrenoceptor antagonist, precursor of the 3-[125I]-derivative	adrenergic receptor antagonist	ADRA1A | ADRA1B | ADRA1D	Non-epigenetic	Non-epigenetic
Heat Shock Treatment		N/A	Heat Shock Treatment	hyperthermia		Non-epigenetic	Non-epigenetic
HH1	11987814	Preclinical	(MC180295) is a novel potent and selective CDK9 inhibitor with an IC50 of 5 nM and is at least 22-fold more selective for CDK9 over other CDKs	cdk inhibitor	CDK9	Non-epigenetic	Non-epigenetic
HHT	285033	Launched	Homoharringtonine, a plant alkaloid, has been reported to suppress protein synthesis and has been approved by the US Food and Drug Administration for the treatment of chronic myeloid leukemia	protein synthesis inhibitor	RPL3	Non-epigenetic	Non-epigenetic
HMN-214	9888590	Phase 1	HMN-214 is a prodrug of HMN-176, which alters the cellular spatial orientation of Plk1	plk inhibitor	PLK1	Non-epigenetic	Non-epigenetic
Hydroxychloroquine	3652	Launched	Hydroxychloroquine (HCQ) is a synthetic oral antimalarial drug that can be used in the study of malaria and autoimmune diseases such as systemic lupus erythematosus and rheumatoid arthritis. Hydroxychloroquine is a potent autophagic flux inhibitor with antiviral activity (such as SARS-CoV-2 virus) that inhibits Toll-like receptor 7/9 (TLR7/9) signaling	antimalarial agent	TLR7 | TLR9	Non-epigenetic	Non-epigenetic
Hydroxyurea	3657	Launched	Hydroxyurea is a cell apoptosis inducer that inhibit DNA synthesis through inhibition of ribonucleotide reductase. Hydroxyurea shows anti-orthopoxvirus activity	ribonucleotide reductase inhibitor	RRM1 | RRM2 | RRM2B	Non-epigenetic	Non-epigenetic
Hypericin	3663	Phase 3	Hypericin is a naturally occurring substance found in Hyperlcurn perforatum L. Hypericin is an inhibitor of PKC (protein kinase C), MAO (monoaminoxidase), dopamine-beta-hydroxylase, reverse transcriptase, telomerase and CYP (cytochrome P450). Hypericin shows antitumor, antiviral, antidepressive activities, and can induce apoptosis	tyrosine kinase inhibitor		Non-epigenetic	Non-epigenetic
Hypericin-based photodynamic therapy		N/A	naturally occurring photosensi-tizer, for photodynamic therapy (PDT) in skin cancer	photodynamic therapy		Non-epigenetic	Non-epigenetic
I-BET151	52912189	Preclinical	(GSK1210151A) is a novel selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 M, 0.25 M, and 0.79 M, respectively.	bromodomain inhibitor	BRD2 | BRD3 | BRD4	Reader	PAHi
i-CRT3		Preclinical	Small cell-permeable oxazole derivative that acts as an inhibitor of both Wnt and β-catenin-responsive transcription	beta catenin inhibitor	CTNNB1 | WNT	Non-epigenetic	Non-epigenetic
Ibrutinib	24821094	Launched	Btk inhibitor with IC50 of 0.5 nM, modestly potent to Bmx, CSK, FGR, BRK, HCK, less potent to EGFR, Yes, ErbB2, JAK3, etc	bruton's tyrosine kinase (btk) inhibitor	BLK | BMX | BTK	Non-epigenetic	Non-epigenetic
Icaritin	5318980	Phase 3	Icaritin (Anhydroicaritin) is a prenylflavonoid derivative from Epimedium brevicornuMaxim. and potently inhibits proliferation of K562 cells (IC50 of 8 µM) and primary CML cells (IC50 of 13.4 µM for CML-CP and 18 µM for CML-BC). Icaritin can regulate MAPK/ERK/JNK and JAK2/STAT3 /AKT signalings, also enhances osteogenesis	ppar receptor antagonist	PDE5A	Non-epigenetic	Non-epigenetic
Icotinib	22024915	Launched	Icotinib (BPI-2009) is a potent and specific EGFR inhibitor with an IC50 of 5 nM; also inhibits mutant EGFRL858R, EGFRL858R/T790M, EGFRT790M and EGFRL861Q. Icotinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups	egfr inhibitor	EGFR	Non-epigenetic	Non-epigenetic
Idarubicin	42890	Launched	Idarubicin is an orally active and potent anthracycline antileukemic agent. Idarubicin inhibits the topoisomerase II interfering with the replication of DNA and RNA transcription. Idarubicin shows induction of DNA damage. Idarubicin inhibits DNA synthesis and of c-myc expression. Idarubicin inhibits the growth of bacteria and yeasts	topoisomerase inhibitor	TOP2A	Non-epigenetic	Non-epigenetic
Idasanutlin	53358942	Phase 3	Idasanutlin (RG7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity	mdm inhibitor	MDM2 | TP53	Non-epigenetic	Non-epigenetic
Idasanutlin + Temozolomide		Phase 3 | Launched	Combination: RG7388 + Temozolomide	dna alkylating agent | mdm inhibitor	MDM2 | MGMT | TOP2A | TP53	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Idelaslib	11625818	Launched	Idelalisib (CAL-101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy	pi3k inhibitor	CCL3 | CCL4 | PIK3CA | PIK3CB | PIK3CD | PIK3CG	Non-epigenetic	Non-epigenetic
IFNy		N/A	Interferon gamma is a Type 1 inflammatory cytokine and the only type II interferon. It has antitumor properties, antiviral activities, and important immunoregulatory functions. The interferon is primarily produced by activated T lymphocytes and natural killer cells	N/A		Non-epigenetic	Non-epigenetic
Ifosfamide	3690	Launched	Ifosfamide is an alkylating chemotherapeutic agent with activity against a wide range of tumors.	dna alkylating agent	CYP2A6 | CYP2B6 | CYP2C18 | CYP2C19 | CYP2C8 | CYP2C9 | CYP3A4 | CYP3A5 | CYP3A7 | PTGS1	Non-epigenetic	Non-epigenetic
IKK 16	9549298	Preclinical	IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM	ikk inhibitor	IKBKB	Non-epigenetic	Non-epigenetic
IL7		N/A	Interleukin 7	N/A		Non-epigenetic	Non-epigenetic
Imatinib	5291	Launched	Multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6μM, 0.1μM and 0.1μM, respectively.	bcr-abl kinase inhibitor | kit inhibitor | pdgfr tyrosine kinase receptor inhibitor	ABCG2 | ABL1 | BCR | CSF1R | CYP2C19 | CYP2C8 | CYP3A5 | DDR1 | KIT | NTRK1 | PDGFRA | PDGFRB | RET	Non-epigenetic	Non-epigenetic
Imatinib + Nilotinib		Launched | Launched	Combination: Imatinib + Nilotinib	abl kinase inhibitor | bcr-abl kinase inhibitor | kit inhibitor | pdgfr tyrosine kinase receptor inhibitor	ABCG2 | ABL1 | BCR | CSF1R | CYP2B6 | CYP2C19 | CYP2C8 | CYP3A5 | DDR1 | KIT | NTRK1 | PDGFRA | PDGFRB | RET	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Imatinib + Nilotinib + GNF2		Launched | Launched | Launched	Combination: Imatinib + Nilotinib + GNF2	abl kinase inhibitor | bcr-abl kinase inhibitor | kit inhibitor | pdgfr tyrosine kinase receptor inhibitor	ABCG2 | ABL1 | BCR | CSF1R | CYP2B6 | CYP2C19 | CYP2C8 | CYP3A5 | DDR1 | KIT | NTRK1 | PDGFRA | PDGFRB | RET	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
IMD-0354	5081913	Phase 1	IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM	ikk inhibitor | nfkb pathway inhibitor	IKBKB	Non-epigenetic	Non-epigenetic
Iniparib	9796068	Phase 3	Iniparib (BSI-201) is an irreversible inhibitor of PARP1, used in the research of triple negative breast cancer	parp inhibitor	PARP1	Non-epigenetic	Non-epigenetic
INK128 (Sapanisertib, TAK228)	45375953	Phase 2	Sapanisertib (INK-128; MLN0128; TAK-228) is an orally available, ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase	mtor inhibitor	MTOR | PIK3CA | PIK3CD | PIK3CG	Non-epigenetic	Non-epigenetic
IPAG	4239764	Preclinical	IPAG is a potent sigma-1 receptor antagonist with a pKi of 4.3. IPAG induces apoptosis	sigma-1 receptor antagonist	SIGMAR1	Non-epigenetic	Non-epigenetic
IRAK1_4i		Preclinical	interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor	interleukin inhibitor | kinase inhibitor	IRAK4	Non-epigenetic	Non-epigenetic
IRAK4i		Preclinical	interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor	interleukin inhibitor | kinase inhibitor	IRAK4	Non-epigenetic	Non-epigenetic
Irinotecan	60838	Launched	Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex	topoisomerase inhibitor	CYP3A5 | TOP1 | TOP1MT	Non-epigenetic	Non-epigenetic
ISCK03	3792751	Preclinical	ISCK03 is a SCF/c-Kit and CD117-specific inhibitor. ISCK03 significantly inhibits c-Kit phosphorylation at 10 μM	cd117-specific inhibitor	CD117	Non-epigenetic	Non-epigenetic
Ispinesib	6851740	Phase 2	Ispinesib is a specific inhibitor of kinesin spindle protein (KSP), with a Ki app of 1.7 nM.	kinesin inhibitor	KIF11	Non-epigenetic	Non-epigenetic
Istradefylline	5311037	Launched	Adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM	adenosine receptor antagonist	ADORA1 | ADORA2A | ADORA2B | ADORA3	Non-epigenetic	Non-epigenetic
Ivermectin	6321424	Launched	Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19	benzodiazepine receptor agonist	CHRNA7 | P2RX7	Non-epigenetic	Non-epigenetic
Ixabepilone	6445540	Launched	Ixabepilone (BMS-247550) is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis	microtubule stabilizing agent	TUBB	Non-epigenetic	Non-epigenetic
Ixazomib	25183872	Launched	Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM)	proteasome inhibitor		Non-epigenetic	Non-epigenetic
JK 184	1069686	Preclinical	JK184 is a potent Hedgehog (Hh) pathway inhibitor with IC50 of 30 nM in mammalian cells	hedgehog pathway inhibitor		Non-epigenetic	Non-epigenetic
JQ1	46907787	Preclinical	JQ1 is a thienotriazolodiazepine and a potent inhibitor of the BET family of bromodomain proteins which include BRD2, BRD3, BRD4, and the testis-specific protein BRDT in mammals.	bromodomain inhibitor	BRD2 | BRD3 | BRD4 | BRDT	Reader	PAHi
JQ1 + Paclitaxel		Preclinical | Launched	Combination: JQ1 + Paclitaxel	bromodomain inhibitor | tubulin polymerization inhibitor	ABCB1 | BCL2 | BRD2 | BRD3 | BRD4 | BRDT | CYP2C8 | MAP2 | MAP4 | MAPT | NR1I2 | TLR4 | TUBA1A | TUBA1B | TUBA1C | TUBA3C | TUBA3D | TUBA3E | TUBA4A | TUBB | TUBB1 | TUBB2A | TUBB2B | TUBB3 | TUBB4A | TUBB4B | TUBB6 | TUBB8	Reader | Non-epigenetic	PAHi | Non-epigenetic
JQ1 + Palbociclib		Preclinical | Launched	Combination: JQ1 + Palbociclib	bromodomain inhibitor | cdk inhibitor	BRD2 | BRD3 | BRD4 | BRDT | CCND3 | CDK4 | CDK6	Reader | Non-epigenetic	PAHi | Non-epigenetic
JTC-801	5311339	Phase 2	JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a Ki value of 8.2 nM	opioid receptor antagonist	OPRL1	Non-epigenetic	Non-epigenetic
KHS101	71304818	Preclinical	Selective inducer of neuronal differentiation; induces neuronal differentiation in cultured hippocampal neural progenitor cells (NPCs) by interacting with TACC3 (EC50 1μM). Suppresses astrocyte formation. Also induces acceleration of neuronal differentiation in the hippocampal dentate gyrusin vivo.	neural stem cell inducer	TACC3	Non-epigenetic	Non-epigenetic
KU-0063794	16736978	Preclinical	Dual-mTOR inhibitor of mTORC1 and mTORC2 with IC50 of 10 nM; no effect on PI3Ks.	mtor inhibitor	MTOR	Non-epigenetic	Non-epigenetic
KW-2449	11427553	Phase 1	Multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1.	abl kinase inhibitor | aurora kinase inhibitor | flt3 inhibitor	ABL1 | AURKA | AURKB | FGFR1 | FLT3	Non-epigenetic	Non-epigenetic
KX2-391	23635314	Launched | Phase 3	Src inhibitor (peptidomimetic class) that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines. Phase 1/2.	protein tyrosine kinase inhibitor | src inhibitor | tubulin polymerization inhibitor	SRC | TUBB	Non-epigenetic	Non-epigenetic
L-Glutamine + Gemcitabine		Launched | Launched	Combination: L-Glutamine + Gemcitabine	ribonucleotide reductase inhibitor	CMPK1 | CTPS1 | GLUL | GPRC6A | PPAT | RRM1 | RRM2 | TYMS	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
L703606 soxalate salt hydrate		Preclinical	Potent and selective non-peptide NK-1 tachykinin receptor antagonist	tachykinin antagonist	TACR1 | TACR2	Non-epigenetic	Non-epigenetic
Lactoferrin	126456119	Preclinical	Lactoferrin (LF), also known as lactotransferrin (LTF), is a multifunctional protein of the transferrin family.	ion transport		Non-epigenetic	Non-epigenetic
Lapatinib	208908	Launched	Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.	egfr inhibitor	CYP3A5 | EGFR | ERBB2	Non-epigenetic	Non-epigenetic
LCL161	24737642	Phase 2	LCL161 is a IAP inhibitor which inhibits XIAP in HEK293 cell and cIAP1 in MDA-MB-231 cell with IC50s of 35 and 0.4 nM, respectively.	xiap inhibitor	BIRC2 | XIAP	Non-epigenetic	Non-epigenetic
LEE011	44631912	Launched	Orally available, and highly specific CDK4/6 inhibitor	cdk inhibitor	CDK4 | CDK6 | JAK3	Non-epigenetic	Non-epigenetic
Lenalidomide	216326	Launched	Derivative of Thalidomide and an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.	anticancer agent	CRBN | TNF	Non-epigenetic	Non-epigenetic
Lenvatinib	9823820	Launched	Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities	fgfr inhibitor | kit inhibitor | pdgfr tyrosine kinase receptor inhibitor | vegfr inhibitor	FGFR1 | FGFR2 | FGFR3 | FGFR4 | FLT1 | FLT4 | KDR | KIT | PDGFB | PDGFRB | RET	Non-epigenetic	Non-epigenetic
Leptomycin B in Ethanol	6917907	Phase 1	Potent and specific nuclear export inhibitor	exportin antagonist	XPO1	Non-epigenetic	Non-epigenetic
Letrozole	3902	Launched	Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer.	aromatase inhibitor	CYP19A1	Non-epigenetic	Non-epigenetic
Leucovorin	135403648	Launched	Folinic acid (Leucovorin) is a biological folic acid and is generally administered along with Methotrexate (MTX) (HY-14519) as a rescue agent to decrease MTX-induced toxicity	folate receptor ligand		Non-epigenetic	Non-epigenetic
Leuprolide	657181	Launched	Leuprolide is an FDA-approved gonadotropin-releasing hormone (GnRH) agonist used for the management of endometriosis, uterine leiomyomata (also known as uterine fibroids), treatment of central precocious puberty in children, and advanced prostate cancer	gonadotropin releasing factor hormone receptor agonist	GNRH1 | GNRHR	Non-epigenetic	Non-epigenetic
Lexibulin	11351021	Phase 2	Lexibulin (CYT-997) is a potent and orally active tubulin polymerisation inhibitor with IC50s of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. Lexibulin induces cell apoptosis and induces mitochondrial ROS generation in GC cells	tubulin polymerization inhibitor	TUBB	Non-epigenetic	Non-epigenetic
Linifanib	11485656	Phase 3	ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells. Phase 3.	pdgfr tyrosine kinase receptor inhibitor | vegfr inhibitor	CSF1 | CSF1R | FLT1 | FLT3 | FLT4 | KDR | KIT | PDGFRA | PDGFRB | RET | TEK	Non-epigenetic	Non-epigenetic
Linsitinib	11640390	Phase 3	Linsitinib (OSI-906) is a potent, selective and orally bioavailable dual inhibitor of the IGF-1 receptor and insulin receptor (IR) with IC50s of 35 and 75 nM, respectively	igf-1 inhibitor	IGF1R | INSR | INSRR	Non-epigenetic	Non-epigenetic
lnc-ASTN1-1		N/A	lncRNA targetting ETV6/RUNX1	lncrna targeting astin1	ASTIN1-1	Non-epigenetic	Non-epigenetic
lnc-NKX2-3-1		N/A	lncRNA targetting ETV6/RUNX1	lncrna targeting nkx2	NKX2	Non-epigenetic	Non-epigenetic
lnc-RTN4R-1		N/A	lncRNA targetting ETV6/RUNX1	lncrna targeting nkx2	RTN4R	Non-epigenetic	Non-epigenetic
lnc-SPARCLE-KO		N/A	SPARCLE knockdown	sparcle expression regulator	SPARCLE	Non-epigenetic	Non-epigenetic
lnc-SPARCLE-OE		N/A	SPARCLE Overexpression	sparcle expression	SPARCLE	Non-epigenetic	Non-epigenetic
lnc-TIMM21-5		N/A	lncRNA targetting ETV6/RUNX1	lncrna targeting nkx2	TIMM21	Non-epigenetic	Non-epigenetic
Lomustine	3950	Launched	Lomustine (CCNU; NSC 79037) is a DNA alkylating agent, with antitumor activity	dna synthesis inhibitor		Non-epigenetic	Non-epigenetic
Lonafarnib	148195	Phase 3	Lonafarnib (Sch66336) is a potent and orally active farnesyl transferase (FTase) inhibitor. Lonafarnib inhibits the activities of H-ras, K-ras and N-ras with IC50 values of 1.9 nM, 5.2 nM and 2.8 nM, respectively. Lonafarnib also has anti-hepatitis delta virus (HDV) activities	farnesyltransferase inhibitor	FNTA | HRAS | KRAS | NRAS	Non-epigenetic	Non-epigenetic
LPS	447388	Preclinical	Lipopolysaccharide treatment	immune response stimulator	IL-10 | IL-6 | TNFA	Non-epigenetic	Non-epigenetic
Luminespib	135539077	Phase 2	HSP90 inhibitor for HSP90α/β with IC50 of 13nM / 21nM, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Phase 1/2.	hsp inhibitor	HSP90AA1 | HSP90AB1	Non-epigenetic	Non-epigenetic
LY-2183240	11507802	Preclinical	Blocker of anandamide uptake (IC50= 270 pM). Inhibits fatty acid amide hydrolase (FAAH) activity (IC50=12.4 nM).	faah inhibitor | faah reuptake inhibitor	FAAH	Non-epigenetic	Non-epigenetic
LY2228820	11570805	Phase 2	Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc	p38 mapk inhibitor	MAPK14	Non-epigenetic	Non-epigenetic
LY2603618	11955855	Phase 2	Rabusertib (LY2603618) is a potent and selective inhibitor of Chk1 with an IC50 of 7 nM	chk inhibitor	CHEK1	Non-epigenetic	Non-epigenetic
Lylamine hydrochloride	16759156	Preclinical		cannabinoid receptor agonist	CNR1	Non-epigenetic	Non-epigenetic
MacOmtOspc		Preclinical	Compounds present in CKI	N/A		Non-epigenetic	Non-epigenetic
Manumycin A	6438330	Preclinical	Competitive cell-permeable Ras farnesyl transferase (Ki = 1.2μM) inhibitor. IB kinase inhibitor. Antibiotic agent. Induces apoptosis. Shows antitumor effectsin vivo.	ras farnesyltransferase inhibitor	FNTA | FNTB	Non-epigenetic	Non-epigenetic
MC180295	137333456	Preclinical	MC180295 ((rel)-MC180295) is a novel potent and selective CDK9 inhibitor with an IC50 of 5 nM and is at least 22-fold more selective for CDK9 over other CDKs.	cdk inhibitor	CDK9	Non-epigenetic	Non-epigenetic
Mechlorethamine	4033	Preclinical	Chlormethine is a nitrogen mustard . It is the prototype of alkylating agents, a group of anticancer chemotherapeutic drugs. It works by binding to DNA, crosslinking two strands and preventing cell duplication. It binds to the N7 nitrogen on the DNA base guanine.	dna alkylating agent	DNA	Non-epigenetic	Non-epigenetic
Megestrol	19090	Launched	Megestrol is a synthetic progestin and used for the treatment of anorexia, cachexia, or an unexplained significant weight loss in patients with an acquired immunodeficiency syndrome diagnosis	progesterone receptor agonist	PGR	Non-epigenetic	Non-epigenetic
Melphalan	460612	Launched	Melphalan (Alkeran, Sarcolysin, L-PAM) is a phenylalanine derivative of nitrogen mustard with antineoplastic activity	dna alkylating agent | dna synthesis inhibitor		Non-epigenetic	Non-epigenetic
Melphalan + NG25		Launched | Preclinical	Combination: Melphalan + NG25	dna alkylating agent | dna inhibitor | tak1 inhibitor	TAK1	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Mercaptopurine	667490	Launched	6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug	immunosuppressant | protein synthesis inhibitor | purine antagonist	HPRT1 | IMPDH1 | IMPDH2 | PPAT	Non-epigenetic	Non-epigenetic
Metaphit	114745	Preclinical	Metaphit is a specific PCPantagonist and site-directed acylating agent of the [3H]phencyclidine binding site in rat brain homogenates[1]. Metaphit prevents PCP-induced locomotor behavior through presynaptic mechanisms[2]	phencyclidine receptor acylator		Non-epigenetic	Non-epigenetic
Methotrexate	126941	Launched	Methotrexate, analog of folic acid, is a nonspecific inhibitor of the dihydrofolate reductase(DHFR) of bacteria and cancerous cells as well as normal cells. It forms an inactive ternary complex with DHFR and NADPH. Methotrexate (MTX) induces apoptosis	dihydrofolate reductase inhibitor	AOX1 | DHFR | FOLR1 | TYMS	Non-epigenetic	Non-epigenetic
Methotrexate + Lactoferrin		Launched | Preclinical	Combination: Methotrexate + Lactoferrin	dihydrofolate reductase inhibitor | ion transport	AOX1 | DHFR | FOLR1 | TYMS	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Methyl Methanesulfonate	4156	Preclinical	Potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM. PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate	midazopyridine diacylglycerol acyltransferase 2 inhibitor	DGAT2	Non-epigenetic	Non-epigenetic
Methylstat	53392493	Preclinical	Methylstat is a potent histone demethylases inhibitor. Methylstat shows anti-proliferative activity with low cytotoxicity. Methylstat induces apoptosis and cell cycle arrest at G0/G1 phase. Methylstat increases the expression of p53 and p21 protein levels. Methylstat inhibits angiogenesis induced by various cytokines. Methylstat can be used as a chemical probe for addressing its role in angiogenesis.	histone demethylase inhibitor	KDM2A | KDM4A | KDM4C | KDM5A | KDM6A | KDM7A | PHF8	Eraser | Reader	HDMi | PMHi
MG-132	462382	Preclinical	Proteasome inhibitor with IC50 of 100 nM, and also inhibits calpain with IC50 of 1.2μM.	proteasome inhibitor	PSMB1	Non-epigenetic	Non-epigenetic
MGCD265	24901704	Preclinical	MGCD-265 analog is a potent and oral active inhibitor of c-Met and VEGFR2 tyrosine kinases, with IC50s of 29 nM and 10 nM, respectively. MGCD-265 analog has significant antitumor activity	vegfr inhibitor	AXL | KDR | MET	Non-epigenetic	Non-epigenetic
Mibefradil dihydrochloride	60662	Withdrawn	Mibefradil dihydrochloride (Ro 40-5967 dihydrochloride) is a calcium channel blocker with moderate selectivity for T-type Ca2+ channels (IC50s of 2.7 μM and 18.6 μM for T-type and L-type currents, respectively)	t-type calcium channel blocker	ANO1 | CACNA1C | CACNA1D | CACNA1F | CACNA1G | CACNA1H | CACNA1I | CACNA1S | CACNB1 | CACNB2 | CACNB3 | CACNB4 | CATSPER1 | CATSPER2 | CATSPER3 | CATSPER4 | SCN2A | SCN4A | SCN5A | SCN9A	Non-epigenetic	Non-epigenetic
Midostaurin	9829523	Launched	Broad spectrum protein kinase inhibitor. Inhibits conventional PKC isoforms (α,β,γ), PDFRβ, VEGFR2, Syk, PKC, Flk-1, Flt3, Cdk1/B, PKA, c-Kit, c-Fgr, c-Src, VEGFR1 and EGFR. Displays potent antitumor activity.	flt3 inhibitor | kit inhibitor | pkc inhibitor	CCNB1 | FLT1 | FLT3 | KDR | KIT | PDGFRB | PRKCA | PRKCG | VEGFA	Non-epigenetic	Non-epigenetic
Mirdametinib	9826528	Phase 2	Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Kiapp of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts	mek inhibitor	MAP2K1 | MAP2K2	Non-epigenetic	Non-epigenetic
Mithramycin	163659	Launched	(Plicamycin) is a selective specificity protein 1 (Sp1) inhibitor. Plicamycin inhibits the growth of various cancers by decreasing Sp1 protein.	rna synthesis inhibitor	SP1	Non-epigenetic	Non-epigenetic
Mithramycin A	163659	Launched	(Plicamycin) is a selective specificity protein 1 (Sp1) inhibitor. Plicamycin inhibits the growth of various cancers by decreasing Sp1 protein.	rna synthesis inhibitor	SP1	Non-epigenetic	Non-epigenetic
Mithramycin A + polym nanoparticles	163659	Launched	(Plicamycin) is a selective specificity protein 1 (Sp1) inhibitor. Plicamycin inhibits the growth of various cancers by decreasing Sp1 protein.	rna synthesis inhibitor	SP1	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Mitomycin	5746	Launched	Mitomycin is a medication used in the treatment of anal carcinoma, bladder carcinoma, breast carcinoma, head and neck malignancies, and some other gastrointestinal carcinomas. It is in the antineoplastic antibiotic class of medications	dna alkylating agent | dna synthesis inhibitor		Non-epigenetic	Non-epigenetic
Mitomycin C	5746	Launched	Mitomycin C (Ametycine) is an antineoplastic antibiotic by inhibiting DNA synthesis, used to treat different cancers. Mitomycin C induces apoptosis in a caspases-dependent and Fas/CD95-independent manner	dna alkylating agent | dna synthesis inhibitor		Non-epigenetic	Non-epigenetic
Mitotane	4211	Launched	Mitotane (2,4′-DDD), an isomer of DDD and derivative of dichlorodiphenyltrichloroethane (DDT), is an antineoplastic agent, can be used to research adrenocortical carcinoma. Mitotane exert its adrenocorticolytic effect at least in part through lipotoxicity induced by intracellular free cholesterol (FC) accumulation. Mitotane can have direct pituitary effects on corticotroph cells. Mitotane can induce CYP3A4 gene expression via steroid and xenobiotic receptor (SXR) activation, and has agent-agent interactions	antineoplastic agent	CYP11A1 | CYP11B1 | CYP3A4 | ESR1	Non-epigenetic	Non-epigenetic
Mitoxantrone	4212	Launched	Topoisomerase II inhibitor; also inhibits protein kinase C (PKC) activity with an IC50 of 8.5 μM.	topoisomerase inhibitor	PIM1 | TOP2A	Non-epigenetic	Non-epigenetic
Mivebresib	71600087	Phase 1	(ABBV-075) Potent and orally active bromodomain and extraterminal domain (BET) bromodomain inhibitor. Mivebresib binds to BRD4 with a Ki of 1.5 nM.	bromodomain inhibitor	BRD4 | MYC | TMPRSS2-ERG	Reader	PAHi
MK-2206	24964624	Phase 2	Inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2	akt inhibitor	AKT1 | AKT2 | AKT3	Non-epigenetic	Non-epigenetic
MK0752	9803433	Phase 1/Phase 2	MK-0752 is a potent, orally active and specific γ-secretase inhibitor, showing dose-dependent reduction of Aβ40 with an IC50 of 5 nM in human SH-SY5Y cells. MK-0752 crosses the blood-brain barrier. MK-0752 reduces newly generated CNS Aβ in vivo	gamma secretase inhibitor		Non-epigenetic	Non-epigenetic
MK2206	24964624	Phase 2	MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC50s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. MK-2206 has anticancer activities	akt inhibitor	AKT1 | AKT2 | AKT3	Non-epigenetic	Non-epigenetic
ML210	49766530	Preclinical	ML-210 is a selective and covalent glutathione peroxidase 4 (GPX4) inhibitor with an EC50 of 30 nM. ML-210 binds the GPX4 selenocysteine residue. ML-210 has anti-cancer activity.	glutathione peroxidase 4 inhibitor	GPX4	Non-epigenetic	Non-epigenetic
MMF	5281078	Launched	Mycophenolate Mofetil (RS 61443, Mycophenolic acid morpholinoethyl ester, CellCept, TM-MMF) is a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase I/II with IC50 of 39 nM and 27 nM, respectively. Mycophenolate Mofetil induces caspase-dependent apoptosis and cell cycle inhibition in multiple myeloma cells	dehydrogenase inhibitor | inositol monophosphatase inhibitor	HCAR2 | IMPDH1 | IMPDH2	Non-epigenetic	Non-epigenetic
MNS	672296	Preclinical	MNS is a potent and selective inhibitor of Src and Syk tyrosine kinases	src inhibitor | syk inhibitor	SRC | SYK	Non-epigenetic	Non-epigenetic
Mocetinostat	9865515	Phase 2	Mocetinostat (MGCD0103) is a potent, orally active and isotype-selective HDAC (Class I/IV) inhibitor with IC50s of 0.15, 0.29, 1.66 and 0.59 μM for HDAC1, HDAC2, HDAC3 and HDAC11, respectively. Mocetinostat shows no inhibition on HDAC4, HDAC5, HDAC6, HDAC7, or HDAC8.	hdac inhibitor	HDAC1 | HDAC11 | HDAC2 | HDAC3	Eraser	HDACi
Momelotinib	25062766	Phase 3	Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3	jak inhibitor	JAK1 | JAK2 | JAK3	Non-epigenetic	Non-epigenetic
Motesanib	11667893	Phase 3	Motesanib (AMG 706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50s of 2 nM/3 nM/6 nM, respectively, and has similar activity against Kit, and is appr 10-fold more selective for VEGFR than PDGFR and Ret	kit inhibitor | pdgfr tyrosine kinase receptor inhibitor | vegfr inhibitor	FLT1 | FLT4 | KDR | KIT | PDGFRA | RET	Non-epigenetic	Non-epigenetic
MS023	92136227	Preclinical	MS023 is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.	protein arginine n-methyltransferase inhibitor	PRMT1 | PRMT3 | PRMT5 | PRMT6	Writer	HMTi
MS023 + GSK591		Preclinical | Preclinical	Combination: MS023 + GSK591	protein arginine n-methyltransferase inhibitor	PRMT1 | PRMT3 | PRMT5 | PRMT6	Writer | Writer	HMTi | HMTi
MST-312	10385095	Preclinical	MST-312 is a telomerase inhibitor. MST-312 is a chemically modified derivative of green tea epigallocatechin gallate (EGCG). MST-312 can be used for the research of cancer, such as multiple myeloma (MM).	telomerase inhibitor	TER	Non-epigenetic	Non-epigenetic
Mycophenolate	446541	Launched	Mycophenolic acid is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 µM. Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid is an immunosuppressive agent. Antiangiogenic and antitumor effects	dehydrogenase inhibitor | inositol monophosphatase inhibitor	IMPDH1 | IMPDH2	Non-epigenetic	Non-epigenetic
N/A		N/A	Not Applicable or No Information	N/A		Non-epigenetic	Non-epigenetic
Navitoclax	24978538	Phase 2	Navitoclax is an orally active, synthetic small molecule and an antagonist of a subset of the B-cell leukemia 2 (Bcl-2) family of proteins with potential antineoplastic activity. Navitoclax selectively binds to apoptosis suppressor proteins Bcl-2, Bcl-XL, and Bcl-w, which are frequently overexpressed in a wide variety of cancers, including those of the lymph, breast, lung, prostate, and colon, and are linked to tumor drug resistance. Inhibition of these apoptosis suppressors prevents their binding to the apoptotic effectors Bax and Bak proteins, thereby triggering apoptotic processes in cells overexpressing Bcl-2, Bcl-XL, and Bcl-w. This eventually reduces tumor cell proliferation.	bcl inhibitor	BCL2 | BCL2L1 | BCL2L2	Non-epigenetic	Non-epigenetic
Navoximod	70914230	Phase 1	Navoximod (GDC-0919; NLG-​919) is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM	indoleamine 2,3-dioxygenase inhibitor	IDO1	Non-epigenetic	Non-epigenetic
Necrosulfonamide	1566236	Preclinical	Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.	mlkl and gasdermin d inhibitor	GSDMD | MLKL	Non-epigenetic	Non-epigenetic
Nelarabine	3011155	Launched	Nelarabine (506U78,Arranon) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.	dna synthesis inhibitor | t cell inhibitor	ADA | POLA1	Non-epigenetic	Non-epigenetic
Neratinib	9915743	Launched	HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM in cell-free assays; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1,c-Raf and c-Met. Phase 3	egfr inhibitor	EGFR | ERBB2 | ERBB4 | KDR	Non-epigenetic	Non-epigenetic
NG25	53340664	Preclinical	NG25 is a novel inhibitor of TAK1 with enzymatic IC50s of 149 and 21.7 nM for TAK1 and MAP4K2 respectivel	tak inhibitor	TAK1	Non-epigenetic	Non-epigenetic
NH125	10436839	Preclinical	NH125 is a potent and selective inhibitor of eukaryotic elongation factor 2 kinase (eEF-2K/CaMKIII), also can induce eEF2 phosphorylation, with an IC50 of 60 nM for eEF-2K	eukaryotic translation elongation factor 2 inhibitor		Non-epigenetic	Non-epigenetic
Niclosamide	4477	Launched	Niclosamide (BAY2353) is an orally active antihelminthic agent used in parasitic infection research. Niclosamide is a STAT3 inhibitor with an IC50 of 0.25 μM in HeLa cells. Niclosamide has biological activities against cancer, inhibits DNA replication in Vero E6 cells.	dna replication inhibitor | stat inhibitor	STAT3	Non-epigenetic	Non-epigenetic
Nigericin	34230	Preclinical	Nigericin is an antibiotic derived from Streptomyces hygroscopicus that act as a K+/H+ ionophore, promoting K+/H+ exchange across mitochondrial membranes. Nigericin shows promising anti-cancer activities through decreasing intracellular pH (pHi), and inactivation of Wnt/β-catenin signals. Nigericin induces pyroptosis through caspase 1/GSDMD in TNBC	nlrp3 inflammasome inducer	NLRP3	Non-epigenetic	Non-epigenetic
Niguldipine hydrochloride	16219720	Preclinical	Norepinephrine hydrochloride (Levarterenol hydrochloride; L-Noradrenaline hydrochloride) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM	adrenergic receptor antagonist	ADRA1A	Non-epigenetic	Non-epigenetic
Nilotinib	644241	Launched	Bcr-Abl inhibitor with IC50 less than 30 nM	abl kinase inhibitor | bcr-abl kinase inhibitor	ABL1 | BCR | CYP2B6 | CYP2C8 | DDR1 | DDR2 | KIT | PDGFRA	Non-epigenetic	Non-epigenetic
Nintedanib	135423438	Launched	Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.	fgfr inhibitor | pdgfr tyrosine kinase receptor inhibitor | vegfr inhibitor	FGFR1 | FGFR2 | FGFR3 | FGFR4 | FLT1 | FLT4 | KDR | LYN | PDGFRA | PDGFRB	Non-epigenetic	Non-epigenetic
Nivolumab		Launched	Nivolumab (anti-PD-1) is a genetically engineered, fully human immunoglobulin (Ig) G4 monoclonal antibody directed against the negative immunoregulatory human cell surface receptor programmed death-1 (PD-1,PCD-1) with immune checkpoint inhibitory and antineoplastic activities	immunotherapy	PD-1	Non-epigenetic	Non-epigenetic
Nivolumab + sPDL1		Launched	Combination: Nivolumab + sPDL1	immunotherapy	PD-1	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
NNC 05-2090 hydrochloride	18782760	Preclinical	NNC 05-2090 hydrochloride is a GABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50< /sub>: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases	gaba uptake inhibitor | gat inhibitor	SLC6A11 | SLC6A12 | SLC6A13	Non-epigenetic	Non-epigenetic
NNC 55-0396	22084904	Preclinical	NNC 55-0396 is a highly selective T-type calcium channel blocker with an IC50 value of 6.8 μM for Cav3.1 T-type channels. NNC 55-0396 can be used for the research of neurological disease research	t-type calcium channel blocker	CATSPER1 | CATSPER2 | CATSPER3 | CATSPER4	Non-epigenetic	Non-epigenetic
Non-targetting LNA GapmeR		N/A	Non-targetting LNA GapmeR	N/A		Non-epigenetic	Non-epigenetic
NSC 632839	5351362	Preclinical	NSC632839 is a nonselective isopeptidase inhibitor, which inhibits USP2, USP7, and SENP2 with EC50s of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively	ubiquitin specific protease inhibitor	SENP2 | USP1 | USP2 | USP7	Non-epigenetic	Non-epigenetic
NSC 663284	379077	Preclinical	NSC 663284 (DA-3003-1) is a potent, cell-permeable, and irreversible Cdc25 dual specificity phosphatase inhibitor, has an IC50 for Cdc25B2 of 0.21 μM. NSC 663284 exhibits mixed competitive kinetics against Cdc25A, Cdc25B(2), and Cdc25C with Ki values of 29, 95, and 89 nM, respectively. NSC 663284 inhibits NSD2 (IC50 of 170 nM) through a direct interaction with the catalytic SET domain (Kd of 370 nM)	cdc inhibitor	CDC25A | CDC25B | CDC25C	Non-epigenetic	Non-epigenetic
NSC 95397	262093	Preclinical	NSC 95397 is a potent, selective Cdc25 dual specificity phosphatase inhibitor (Ki=32 nM (Cdc25A), 96 nM (Cdc25B), 40 nM (Cdc25C); IC50=22.3 nM (human Cdc25A), 56.9 nM (human Cdc25C), 125 nM (Cdc25B)). NSC 95397 inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and suppresses proliferation and induces apoptosis in colon cancer cells through MKP-1 and ERK1/2 pathway	cdc inhibitor	CASP3 | CDC25A | CDC25B	Non-epigenetic	Non-epigenetic
Nutlin 3	216345	Preclinical	Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM in a cell-free assay; stabilizes p73 in p53-deficient cells.	mdm inhibitor	MDM2 | TP53	Non-epigenetic	Non-epigenetic
NVP-2	66937006	Preclinical	NVP-2 is a potent and selective ATP-competitive cyclin dependent kinase 9 (CDK9) probe, inhibits CDK9/CycT activity with an IC50 of 0.514 nM. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC50 values of 0.584 µM, 0.706 µM, and 0.605 µM, respectively. NVP-2 induces cell apoptosis.	cdk inhibitor	CDK1 | CDK16 | CDK2 | CDK9	Non-epigenetic	Non-epigenetic
NVP-231	4096211	Preclinical	Ceramide kinase (CerK) inhibitor (IC50= 12 nMin vitro). Displays selectivity for CerK over sphingosine kinases (IC50>100μM) and other lipid kinases	ceramidase inhibitor	CERK	Non-epigenetic	Non-epigenetic
Obatoclax	11404337	Phase 3	Antagonist of Bcl-2 with Ki of 0.22μM, can assist in overcoming MCL-1 mediated resistance to apoptosis. Phase 1/2.	bcl inhibitor	BCL2 | BCL2L1 | MCL1	Non-epigenetic	Non-epigenetic
Obatoclax mesylate	16681698	Phase 3	Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity	bcl inhibitor	BCL2 | BCL2L1 | MCL1	Non-epigenetic	Non-epigenetic
Olaparib	23725625	Launched	Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator	parp inhibitor	PARP1 | PARP2 | PARP3	Non-epigenetic	Non-epigenetic
Omacetaxine	65305	Preclinical	Homoharringtonine (Omacetaxine mepesuccinate;HHT) is a cytotoxic alkaloid with antitumor properties which acts by inhibiting translation elongation	protein synthesis inhibitor		Non-epigenetic	Non-epigenetic
OmtOspc		Preclinical	Compounds present in CKI	cell proliferation inhibitor		Non-epigenetic	Non-epigenetic
Onalespib	11955716	Phase 2	Selective potent Hsp90 inhibitor with IC50of 18 nM in A375 cells, displays a long duration of anti-tumor activity.	hsp inhibitor	HSP90AA1	Non-epigenetic	Non-epigenetic
Oprozomib	25067547	Phase 1/Phase 2	Oprozomib (PR-047) is an orally bioavailable and selective peptide epoxyketone proteasome inhibitor with IC50s of 36 and 82 nM for proteasome (β5) and immunoproteasome (LMP7), respectively. Oprozomib (ONX 0912) induces apoptosis in MM cells	proteasome inhibitor		Non-epigenetic	Non-epigenetic
Orteronel	9796590	Phase 3	Orteronel (TAK-700) is a highly selective inhibitor of human 17,20-lyase (CYP17) with IC50 of 38 nM, and exhibits >1000-fold selectivity over other CYPs such as 11-hydroxylase and CYP3A4	androgen biosynthesis inhibitor | androgen receptor antagonist | cytochrome p450 inhibitor	CYP17A1	Non-epigenetic	Non-epigenetic
Osimertinib	71496458	Launched	Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer	egfr inhibitor	EGFR	Non-epigenetic	Non-epigenetic
OTS964	67448186	Preclinical	OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.	cdk inhibitor | topk inhibitor	CDK11 | PBK	Non-epigenetic	Non-epigenetic
Oxaliplatin	5310940	Launched	Oxaliplatin is a DNA synthesis inhibitor. Oxaliplatin causes DNA crosslinking damage, prevents DNA replication and transcription and induces apoptosis. Oxaliplatin can be used for cancer research	dna inhibitor	DNA	Non-epigenetic	Non-epigenetic
PAC-1	135421197	Phase 1	Procaspase-3 activator with EC50 of 0.22μM and the first small molecule known to directly activate procaspase-3 to caspase-3.	caspase activator	CASP3	Non-epigenetic	Non-epigenetic
Paclitaxel	36314	Launched	Microtubule polymer stabilizer with anIC50of 0.1 pM for human endothelial cells.	tubulin polymerization inhibitor	ABCB1 | BCL2 | CYP2C8 | MAP2 | MAP4 | MAPT | NR1I2 | TLR4 | TUBA1A | TUBA1B | TUBA1C | TUBA3C | TUBA3D | TUBA3E | TUBA4A | TUBB | TUBB1 | TUBB2A | TUBB2B | TUBB3 | TUBB4A | TUBB4B | TUBB6 | TUBB8	Non-epigenetic	Non-epigenetic
Pacritinib	46216796	Phase 3	Pacritinib (SB1518) is a potent inhibitor of both wild-type JAK2 (IC50=23 nM) and JAK2V617F mutant (IC50=19 nM). Pacritinib also inhibits FLT3 (IC50=22 nM) and its mutant FLT3D835Y (IC50=6 nM)	flt3 inhibitor | jak inhibitor	CDK2 | FLT3 | JAK1 | JAK2 | JAK3	Non-epigenetic	Non-epigenetic
Palbociclib	5330286	Launched	Palbociclib (PD 0332991) is a selective CDK4 and CDK6 inhibitor with IC50s of 11 and 16 nM, respectively. Palbociclib has the potential for ER-positive and HER2-negative breast cancer research	cdk inhibitor	CCND3 | CDK4 | CDK6	Non-epigenetic	Non-epigenetic
Palbociclib + TAK228		Launched	Combination: Palbociclib + TAK228	cdk inhibitor | mtor inhibitor	CCND3 | CDK4 | CDK6 | MTOR	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Panobinostat	6918837	Launched	Broad-spectrum HDAC inhibitor with IC50 of 5 nM. Phase 3.	hdac inhibitor	HDAC1 | HDAC2 | HDAC3 | HDAC4 | HDAC6 | HDAC7 | HDAC8 | HDAC9	Eraser	HDACi
Panobinostat + Azacitidine		Launched	Combination: Panobinostat and Azacitidine	dna methyltransferase inhibitor | hdac inhibitor	DNMT1 | DNMT3A | HDAC1 | HDAC2 | HDAC3 | HDAC4 | HDAC6 | HDAC7 | HDAC8 | HDAC9	Eraser | Writer	DNMTi | HDACi
Parbendazole	26596	Preclinical	Potent inhibitor of mutubule assembly and functions	tubulin polymerization inhibitor	TUBB	Non-epigenetic	Non-epigenetic
Parthenolide	7251185	Preclinical	Sesquiterpene lactone which occurs naturally in the plant fever few (Tanacetum parthe-nium). Promotes the ubiquitination of MDM2 and activates p53 cellular functions.	nfkb pathway inhibitor	ADIPOR2 | IKBKB | RELA	Non-epigenetic	Non-epigenetic
Pazopanib	10113978	Launched	Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively	kit inhibitor | pdgfr tyrosine kinase receptor inhibitor | vegfr inhibitor	BRAF | CSF1R | CYP2B6 | CYP2C8 | CYP2E1 | DDR2 | FGF1 | FGFR1 | FGFR3 | FLT1 | FLT4 | ITK | KDR | KIT | PDGFRA | PDGFRB | SH2B3	Non-epigenetic	Non-epigenetic
PC3-Docetaxel-resistant		N/A		N/A		Non-epigenetic	Non-epigenetic
PD 184161	9937619	Preclinical	PD184161 is an orally active MEK inhibitor. PD184161 inhibits MEK activity (IC50=10-100 nM) in a time- and concentration-dependent manner. PD184161 inhibits cell proliferation and induces apoptosis. PD184161 produces depressive-like behavior	mek inhibitor	MEK	Non-epigenetic	Non-epigenetic
PD173074	1401	Preclinical	PD173074 is a potent FGFR1 inhibitor with an IC50 of 25 nM and also inhibits VEGFR2 with an IC50 of 100-200 nM, showing 1000-fold selectivity for FGFR1 over PDGFR and c-Src	fgfr inhibitor | vegfr inhibitor	FGFR1 | FGFR2 | FGFR3 | FGFR4 | FLT1 | FLT4 | KDR | PDGFRA | PDGFRB	Non-epigenetic	Non-epigenetic
Pemetrexed	135410875	Launched	Pemetrexed (LY231514) is an antifolate, the Ki values of the pentaglutamate of Pemetrexed (LY231514) are 1.3, 7.2, and 65 nM for inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT), respectively	dihydrofolate reductase inhibitor | thymidylate synthase inhibitor	ATIC | DHFR | GART | SLC22A8 | TYMS	Non-epigenetic	Non-epigenetic
Pentostatin	439693	Launched	Pentostatin (CI-825; Deoxycoformycin) is an irreversible inhibitor of adenosine deaminase with Ki of 2.5 pM	adenosine deaminase inhibitor | adenosine deaminase inhibitor, ribonucleotide reductase inhibitor | ribonucleotide reductase inhibitor	ADA	Non-epigenetic	Non-epigenetic
Perifosine	148177	Phase 3	Perifosine is an oral Akt inhibitor which inhibits proliferation of different tumor cell lines with IC50s of 0.6-8.9 μM	akt inhibitor	AKT1 | PIK3CA	Non-epigenetic	Non-epigenetic
Pervanadate	24978557	Preclinical	Pervanadate is a protein tyrosine phosphatase inhibitor that is commonly used to increase tyrosine phosphorylation in cells. When cells are treated with pervanadate for 30 minutes they undergo significant tyrosine phosphorylation, as shown by western blotting using anti-Phosphotyrosine.	tyrosine phosphatase inhibitor	PTPN1 | PTPN11 | PTPN2	Non-epigenetic	Non-epigenetic
Pervanadate + IFNy		Preclinical	Combination: Pervanadate + IFNy	ifng | tyrosine phosphatase inhibitor	PTPN1 | PTPN11 | PTPN2	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Pevonedistat	16720766	Phase 3	Pevonedistat (MLN4924) is a potent and selective NEDD8-activating enzyme (NAE) inhibitor with an IC50 of 4.7 nM	nedd activating enzyme inhibitor	NAE1 | UBA3	Non-epigenetic	Non-epigenetic
PF-04691502	25033539	Phase 2	PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with Kis of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively	mtor inhibitor | pi3k inhibitor	MTOR | PIK3CA | PIK3CB | PIK3CD | PIK3CG	Non-epigenetic	Non-epigenetic
PF-3758309	25227462	Phase 1	ATP-competitive, pyrrolopyrazole inhibitor of PAK4 withIC50of 1.3 nM	p21 activated kinase inhibitor	PAK4	Non-epigenetic	Non-epigenetic
PF-573228	11612883	Preclinical	ATP-competitive inhibitor of FAK with IC50 of 4 nM, 50- to 250-fold selective for FAK than Pyk2, CDK1/7 and GSK-3β.	focal adhesion kinase inhibitor	CDK1 | CDK2 | CDK7 | GSK3B | IKBKB	Non-epigenetic	Non-epigenetic
PHA-665752	10461815	Preclinical	ATP-competitive c-Met inhibitor withIC50of 9 nM, >50-fold selectivity for c-Met than RTKs or STKs.	c-met inhibitor	MET	Non-epigenetic	Non-epigenetic
Phenelzine	3675	Launched	Phenelzine is a monoamine oxidase inhibitor used to treat atypical, nonendogenous, or neurotic depression	monoamine oxidase inhibitor	ABAT | AOC3 | GAD2 | GPT | GPT2 | MAOA | MAOB | SLC6A2 | SLC6A3 | SLC6A4	Non-epigenetic	Non-epigenetic
Phleomycin	72511	Preclinical	Phleomycin is an anticancer glycopeptide antibiotic found in Streptomyces verticillus, which cause DNA cleavage. Phleomycin binds and intercalates DNA to damage the integrity of the double helix, which is similar to Bleomycin (HY-17565A)	bacterial dna inhibitor		Non-epigenetic	Non-epigenetic
Phorbol myristate acetate	27924	Phase 2	Phorbol 12-myristate 13-acetate (PMA), a phorbol ester, is a dual SphK and protein kinase C (PKC) activator. Phorbol 12-myristate 13-acetate is a NF-κB activator. Phorbol 12-myristate 13-acetate induces differentiation in THP-1 cells	pkc activator	CD4 | KCNT2 | TRPV4	Non-epigenetic	Non-epigenetic
PI-103	9884685	Preclinical	PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy	mtor inhibitor | pi3k inhibitor	MTOR | PIK3CA | PIK3CB | PIK3CD | PIK3CG | PRKDC	Non-epigenetic	Non-epigenetic
Picoplatin	177358	Preclinical	Picoplatin (AMD473) is a platinum-based antineoplastic agent. Picoplatin is specifically to circumvent thiol-mediated drug resistance by sterically hindering its reaction with glutathione (GSH) while still retaining the ability to form cytotoxic lesions with DNA	antineoplastic agent	GSH	Non-epigenetic	Non-epigenetic
Pictilisib	17755052	Phase 2	Inhibitor of PI3Kα and δ with IC50 of 3 nM in cell-free assays, with modest selectivity against PI3Kβ (11-fold) and PI3Kγ (25-fold). Phase 2.	pi3k inhibitor	PIK3CA | PIK3CB | PIK3CD | PIK3CG	Non-epigenetic	Non-epigenetic
PIK-75	10275789	Preclinical	PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis	dna protein kinase inhibitor | pi3k inhibitor	PIK3CA | PIK3CB | PIK3CD | PIK3CG | PRKDC	Non-epigenetic	Non-epigenetic
Pilaralisib	56599306	Phase 2	Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ	pi3k inhibitor		Non-epigenetic	Non-epigenetic
Pimasertib	44187362	Phase 2	Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor	mek inhibitor	MAP2K1 | MAP2K2	Non-epigenetic	Non-epigenetic
Pinometostat	57345410	Phase 1	Pinometostat (EPZ-5676) is a potent DOT1L histone methyltransferase inhibitor with a Ki of 80 pM.	histone lysine methyltransferase inhibitor	DOT1L	Writer	HMTi
Piperlongumine	637858	Preclinical	Piperlongumine is a alkaloid, possesses ant-inflammatory, antibacterial, antiangiogenic, antioxidant, antitumor, and antidiabetic activities. Piperlongumine induces ROS, and induces apoptosis in cancer cell lines. Piperlongumine shows anti-cardiac fibrosis activity, suppresses myofibroblast transformation via suppression of the ERK1/2 signaling pathway. Piperlongumin could be used in the study of migrasome.	activator of transcription 3 | extracellular signal-regulated kinase | janus kinases signal transducer | mtor inhibitor | nuclear factor-kappa b | phosphatidylinositol-3-kinase kinase inhibitor	ERK | JAK | MTOR | PI3K | STAT3	Non-epigenetic	Non-epigenetic
Pipobroman	4842	Launched	Pipobroman is a bromide derivative of piperazine and acts as an alkylating agent. Pipobroman plays its role by inhibiting DNA and RNA polymerase or by reducing pyrimidine nucleotide incorporation into DNA. Pipobroman can be used for the cancer research, including polycythemia vera, myeloproliferative neoplasm, and AML et.al	dna alkylating agent		Non-epigenetic	Non-epigenetic
Pirarubicin	11296583	Launched	Pirarubicin is an anthracycline antibiotics, acts as a topoisomerase II inhibitor, and is a widely used for treatment of various cancers, in particular, solid tumors.	topoisomerase inhibitor	TOP2A	Non-epigenetic	Non-epigenetic
Pixantrone	134019	Launched	Pixantrone (BBR 2778) dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity	topoisomerase inhibitor	TOP2A	Non-epigenetic	Non-epigenetic
Plinabulin	9949641	Phase 3	Plinabulin (NPI-2358) is a vascular disrupting agen (VDA) against tubulin-depolymerizing with an IC50 of 9.8 nM against HT-29 cells. Plinabulin binds the colchicine binding site of β-tubulin preventing polymerization and has potent inhibitory to tumor cell	tubulin polymerization inhibitor		Non-epigenetic	Non-epigenetic
Pluripotin	12003241	Preclinical	Pluripotin is a dual inhibitor of ERK1 and RasGAP with KDs of 98 nM and 212 nM, respectively. Pluripotin also inhibits RSK1, RSK2, RSK3, and RSK4 with IC50s of 0.5, 2.5, 3.3, and 10.0 μM, respectively.	erk inhibitor | rasgap inhibitor	ERK1 | RasGAP | RSK1 | RSK2 | RSK3 | RSK4	Non-epigenetic	Non-epigenetic
Podofilox	10607	Launched	Podofilox (Podophyllotoxin) is a potent inhibitor of microtubule assembly and DNA topoisomerase II	microtubule inhibitor | tubulin polymerization inhibitor	IGF1R | TOP2A | TUBA4A | TUBB	Non-epigenetic	Non-epigenetic
Pomalidomide	134780	Launched	Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors	angiogenesis inhibitor | tumor necrosis factor production inhibitor	CRBN | CYP2C19 | TNF	Non-epigenetic	Non-epigenetic
Ponatinib	24826799	Launched	Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.	bcr-abl kinase inhibitor | flt3 inhibitor | pdgfr tyrosine kinase receptor inhibitor	ABL1 | BCR | CYP2C8 | CYP3A5 | FGF2 | FGFR1 | FGFR2 | FGFR3 | FGFR4 | FLT1 | FLT3 | KDR | KIT | LCK | LYN | PDGFRA | RET | SRC | TEK	Non-epigenetic	Non-epigenetic
Ponatinib + Dactolisib		Launched | Phase 3	Combination: (Ponatinib) and (Dactolisib). Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively. AND Dactolisib (BEZ235) is an orally active and dual pan-class I PI3K and mTOR kinase inhibitor with IC50s of 4 nM/5 nM/7 nM/75 nM, and 20.7 nM for p110α/p110γ/p110δ/p110β and mTOR, respectively. Dactolisib (BEZ235) inhibits both mTORC1 and mTORC2	bcr-abl kinase inhibitor | flt3 inhibitor | mtor inhibitor | pdgfr tyrosine kinase receptor inhibitor | pi3k inhibitor	ABL1 | ATR | BCR | CYP2C8 | CYP3A5 | FGF2 | FGFR1 | FGFR2 | FGFR3 | FGFR4 | FLT1 | FLT3 | KDR | KIT | LCK | LYN | MTOR | PDGFRA | PIK3CA | PIK3CB | PIK3CD | PIK3CG | RET | SRC | TEK	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
PP121	24905142	Preclinical	PP121 is a multi-targeted kinase inhibitor with IC50s of 10, 60, 12, 14, 2 nM for mTOR, DNK-PK, VEGFR2, Src, PDGFR, respectively	protein tyrosine kinase inhibitor	ABL1 | EGFR | HCK | KDR | MTOR | PDGFRA | PIK3CA | PIK3CB | PIK3CD | PIK3CG | PRKDC | SRC	Non-epigenetic	Non-epigenetic
Pracinostat	49855250	Phase 3	Pracinostat is a potent histone deacetylase (HDAC) inhibitor, with IC50s of 40-140 nM, used for cancer research. Pracinostat also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2) hydrolase activity with an EC50 below 10 nM	hdac inhibitor	HDAC1 | HDAC10 | HDAC2 | HDAC3 | HDAC4 | HDAC5 | HDAC6 | HDAC9	Eraser	HDACi
Pralatrexate	148121	Launched	Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment. Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups	dihydrofolate reductase inhibitor	DHFR | SLC19A1	Non-epigenetic	Non-epigenetic
Prednisone	5865	Launched	Prednisone (NSC-10023, Adasone) is a synthetic corticosteroid agent that is particularly effective as an immunosuppressant compound	glucocorticoid receptor agonist	HSD11B1 | NR3C1	Non-epigenetic	Non-epigenetic
Prexasertib	46700756	Phase 2	Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity.	chk inhibitor	CHEK1	Non-epigenetic	Non-epigenetic
Prexasertib + Gemcitabine		Phase 2	Combination: Prexasertib + Gemcitabine	chk inhibitor | ribonucleotide reductase inhibitor	CHEK1 | CMPK1 | RRM1 | RRM2 | TYMS	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Prinomastat	466151	Phase 3	Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity	matrix metalloprotease inhibitor	MMP1 | MMP2 | MMP3 | MMP9	Non-epigenetic	Non-epigenetic
Procarbazine	4915	Launched	Procarbazine Hydrochloride is an orally active alkylating agent, with anticancer activity. Procarbazine Hydrochloride can be used in Hodgkin's disease research	monoamine oxidase inhibitor		Non-epigenetic	Non-epigenetic
Propranolol	4946	Launched	Propranolol is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM. Propranolol is used for the study of hypertension, pheochromocytoma, myocardial infarction, cardiac arrhythmias, angina pectoris, and hypertrophic cardiomyopathy	adrenergic receptor antagonist	ADRB1 | ADRB2	Non-epigenetic	Non-epigenetic
Proscillaridin A	5284613	Launched	Potent poison of topoisomerase I/II activity with IC50 values of 30 nM and 100 nM, respectively.	topoisomerase inhibitor	TOP2A | TOP2B	Non-epigenetic	Non-epigenetic
PX12	219104	Phase 2	PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1 (Trx-1); inhibits the growth of MCF-7 and HT-29 cells with IC50 values of 1.9 and 2.9 μM, respectively	thioredoxin inhibitor	CNR1 | TXN | TXNRD1 | TXNRD2	Non-epigenetic	Non-epigenetic
Pyrrolidinedithiocarbamate ammonium	517348	Preclinical	Pyrrolidinedithiocarbamate ammonium (Ammonium pyrrolidinedithiocarbamate) is a selective and blood-brain barrier (BBB) permeable NF-κB inhibitor.	nfkb pathway inhibitor	NFKB1	Non-epigenetic	Non-epigenetic
Quinacrine dihydrochloride	6239	Preclinical	Quinacrine (Mepacrine) dihydrochloride is an orally bioavailable antimalarial agent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppresses NF-κB and activate p53 signaling, which results in the induction of the apoptosis	nfkb pathway inhibitor | p53 activator	NFKB1 | TP53	Non-epigenetic	Non-epigenetic
Quizartinib	24889392	Phase 3	Quizartinib (AC220) is an orally active, highly selective and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. Quizartinib inhibits wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells with IC50s of 4.2 and 1.1 nM, respectively. Quizartinib can be linked to the VHL ligand via an optimized linker to form a PROTAC FLT3 degrader. Quizartinib induces apoptosis	flt3 inhibitor	CSF1R | FLT3 | KIT | PDGFRA | PDGFRB | RET	Non-epigenetic	Non-epigenetic
R-CR8	90488866	Preclinical	(R)​-​CR8 (CR8), a second-generation analog of Roscovitine, is a potent CDK1/2/5/7/9 inhibitor. (R)​-​CR8 inhibits CDK1/cyclin B (IC50=0.09 μM), CDK2/cyclin A (0.072 μM), CDK2/cyclin E (0.041 μM), CDK5/p25 (0.11 μM), CDK7/cyclin H (1.1 μM), CDK9/cyclin T (0.18 μM) and CK1δ/ε (0.4 μM). (R)​-​CR8 induces apoptosis and has neuroprotective effect. (R)-CR8 acts as a molecular glue degrader that depletes cyclin K	cdk inhibitor	CCNA2 | CCNE1 | CCNH | CCNT1 | CDK1 | CDK2 | CDK5 | CDK7 | CDK9	Non-epigenetic	Non-epigenetic
RAF265	11656518	Phase 2	RAF265 is a potent and orally active RAF/VEGFR2 inhibitor	raf inhibitor | vegfr inhibitor	BRAF | KDR | KIT | PDGFRB | RAF1	Non-epigenetic	Non-epigenetic
Raji Co-culture		N/A	Co-culture of Burkitts Lymphoma cell line	N/A		Non-epigenetic	Non-epigenetic
Raloxifene	5035	Launched	Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research.	estrogen receptor antagonist | selective estrogen receptor modulator (serm)	ACVRL1 | ENG | ESR1 | ESR2	Non-epigenetic	Non-epigenetic
Raltitrexed	135400182	Launched	Raltitrexed is an antimetabolite agent used in chemotherapy, acting by inhibiting thymidylate synthase	thymidylate synthase inhibitor	FPGS | TYMS	Non-epigenetic	Non-epigenetic
Rapamycin	5284616	Launched	Rapamycin (Sirolimus; AY 22989) is a potent and specific mTOR inhibitor with an IC50 of 0.1 nM in HEK293 cells. Rapamycin binds to FKBP12 and specifically acts as an allosteric inhibitor of mTORC1. Rapamycin is an autophagy activator, an immunosuppressant.	mtor inhibitor	CCR5 | FKBP1A | MTOR	Non-epigenetic	Non-epigenetic
Refametinib	44182295	Phase 2	Refametinib (BAY 869766; RDEA119) is an orally available, potent, non-ATP-competitive, selective, allosteric MEK1/MEK2 inhibitor with IC50s of 19 nM and 47 nM, respectively	mek inhibitor	MAP2K1 | MAP2K2	Non-epigenetic	Non-epigenetic
Regorafenib	11167602	Launched	Regorafenib (BAY 73-4506) is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib shows very robust antitumor and antiangiogenic activity	fgfr inhibitor | kit inhibitor | pdgfr tyrosine kinase receptor inhibitor | raf inhibitor | ret tyrosine kinase inhibitor | vegfr inhibitor	ABL1 | BRAF | CYP2B6 | CYP2C19 | CYP2C8 | DDR2 | EPHA2 | FGF2 | FGFR1 | FGFR2 | FLT1 | FLT4 | FRK | KDR | KIT | MAPK11 | NTRK1 | PDGFRA | PDGFRB | RAF1 | RET | TEK	Non-epigenetic	Non-epigenetic
Regorafenib + AZD4547 + Vatalanib		Launched | Phase 2/Phase 3 | Phase 3	Combination: Regorafenib + AZD4547 + Vatalanib	fgfr inhibitor | kit inhibitor | pdgfr tyrosine kinase receptor inhibitor | raf inhibitor | ret tyrosine kinase inhibitor | vegfr inhibitor	ABL1 | BRAF | CYP19A1 | CYP2B6 | CYP2C19 | CYP2C8 | DDR2 | EGFR | EPHA2 | FGF2 | FGFR1 | FGFR2 | FGFR3 | FGFR4 | FLT1 | FLT4 | FRK | IGF1R | KDR | KIT | MAPK11 | NTRK1 | PDGFRA | PDGFRB | RAF1 | RET | TEK	Non-epigenetic | Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic | Non-epigenetic
Regorafenib + GDC0994		Launched | Phase 1	Combination: Regorafenib + GDC0994	erk1 and erk2 phosphorylation inhibitor | fgfr inhibitor | kit inhibitor | pdgfr tyrosine kinase receptor inhibitor | raf inhibitor | ret tyrosine kinase inhibitor | vegfr inhibitor	ABL1 | BRAF | CYP2B6 | CYP2C19 | CYP2C8 | DDR2 | EPHA2 | FGF2 | FGFR1 | FGFR2 | FLT1 | FLT4 | FRK | KDR | KIT | MAPK1 | MAPK11 | MAPK3 | NTRK1 | PDGFRA | PDGFRB | RAF1 | RET | TEK	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Regorafenib + Selumetinib		Launched | Phase 3	Combination: Regorafenib + Selumetinib	fgfr inhibitor | kit inhibitor | mek inhibitor | pdgfr tyrosine kinase receptor inhibitor | raf inhibitor | ret tyrosine kinase inhibitor | vegfr inhibitor	ABL1 | BRAF | CYP2B6 | CYP2C19 | CYP2C8 | DDR2 | EPHA2 | FGF2 | FGFR1 | FGFR2 | FLT1 | FLT4 | FRK | KDR | KIT | MAP2K1 | MAP2K2 | MAPK11 | NTRK1 | PDGFRA | PDGFRB | RAF1 | RET | TEK	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Regorafenib + Vemurafenib		Launched | Launched	Combination: Regorafenib + Vemurafenib + GDC0994	fgfr inhibitor | kit inhibitor | pdgfr tyrosine kinase receptor inhibitor | raf inhibitor | ret tyrosine kinase inhibitor | vegfr inhibitor	ABL1 | BRAF | CYP2B6 | CYP2C19 | CYP2C8 | CYP3A4 | CYP3A5 | DDR2 | EPHA2 | FGF2 | FGFR1 | FGFR2 | FLT1 | FLT4 | FRK | KDR | KIT | MAPK11 | NTRK1 | PDGFRA | PDGFRB | RAF1 | RET | TEK	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Regorafenib + Vemurafenib + GDC0994		Launched | Launched | Phase 1	Combination: Regorafenib + Vemurafenib + GDC0994	erk1 and erk2 phosphorylation inhibitor | fgfr inhibitor | kit inhibitor | pdgfr tyrosine kinase receptor inhibitor | raf inhibitor | ret tyrosine kinase inhibitor | vegfr inhibitor	ABL1 | BRAF | CYP2B6 | CYP2C19 | CYP2C8 | CYP3A4 | CYP3A5 | DDR2 | EPHA2 | FGF2 | FGFR1 | FGFR2 | FLT1 | FLT4 | FRK | KDR | KIT | MAPK1 | MAPK11 | MAPK3 | NTRK1 | PDGFRA | PDGFRB | RAF1 | RET | TEK	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Resminostat	11609955	Phase 2	Resminostat hydrochloride is a potent inhibitor of HDAC1, HDAC3 and HDAC6, with mean IC50 values of 42.5, 50.1, 71.8 nM, respectively, and shows less potent activities against HDAC8, with an IC50 of 877 nM	hdac inhibitor	HDAC1 | HDAC2 | HDAC3 | HDAC6 | HDAC8	Eraser	HDACi
Resveratrol	445154	Launched	Stimulates mitochondrial growth/metabolism via SIRT1/AMPK; pan HDAC inhibitor	cytochrome p450 inhibitor | sirt activator	APOA1 | BACE1 | CSNK2A1 | MAOA | NQO2 | PTGS1 | PTGS2 | SCN5A | SIRT1 | TXNRD1 | TXNRD2 | XDH	Eraser | Non-epigenetic	HDACi | Non-epigenetic
Retinoic Acid	444795	Launched	Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.	retinoid receptor agonist | retinoid receptor ligand	ALDH1A1 | ALDH1A2 | GPRC5A | NR0B1 | NR2C2 | PPARD | RARA | RARB | RARG | RARRES1 | RORB | RORC | RXRB | RXRG	Non-epigenetic	Non-epigenetic
Ribociclib	44631912	Launched	Ribociclib (LEE01) is a highly specific CDK4/6 inhibitor with IC50 values of 10 nM and 39 nM, respectively, and is over 1,000-fold less potent against the cyclin B/CDK1 complex.	cdk inhibitor	CDK4 | CDK6 | JAK3	Non-epigenetic	Non-epigenetic
Rigosertib	6918736	Phase 3	Non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Phase 3.	cell cycle inhibitor | plk inhibitor	MCL1 | PLK1	Non-epigenetic	Non-epigenetic
Rituximab	168009840	Launched	Rituximab is an anti-CD20 chimeric monoclonal antibody used for research of certain autoimmune diseases and cancer.	chimeric monoclonal antibody	CD20	Non-epigenetic	Non-epigenetic
Riviciclib hydrochloride	23643975	Phase 2	Riviciclib hydrochloride (P276-00) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively. Riviciclib hydrochloride (P276-00) shows antitumor activity on cisplatin-resistant cells	cdk inhibitor	CDK1 | CDK4 | CDK9	Non-epigenetic	Non-epigenetic
Ro 08-2750	17756791	Preclinical	Ro 08-2750 is a non-peptide and reversible nerve growth factor (NGF) inhibitor which binds to NGF, and with an IC50 of ~ 1 µM. Ro 08-2750 inhibits NGF binding to p75NTR selectively over TRKA. Ro 08-2750 is a selective MSI RNA-binding activity inhibitor, with an IC50 of 2.7 μM.	ngf binding inhibitor	NGF | NGFR	Non-epigenetic	Non-epigenetic
Ro 106-9920	3906779	Preclinical	Ro 106-9920 is a potent inhibitor of NF-kappaB. Ro 106-9920 has the potential for the research of tumor and cancer diseases	nfkb pathway inhibitor		Non-epigenetic	Non-epigenetic
Ro 31-8220 mesylate	11628205	Preclinical	Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7. Ro 31-8220 mesylate can also inhibit the expression of MKP-1, induce the expression of c-Jun, and activate JNK, and these effects possess pharmacological properties independent of PKC.	mapk inhibitor | pkc inhibitor	MAPKAP-K1b | MKP-1 | MSK1 | PRKCA | PRKCB | PRKCD | PRKCE | PRKCH | PRKCQ | S6K1	Non-epigenetic	Non-epigenetic
RO4929097	49867930	Phase 2	RO4929097 (RG-4733) is a γ secretase inhibitor with IC50 of 4 nM, inhibiting cellular processing of Aβ40 and Notch with EC50 of 14 nM and 5 nM, respectively	gamma secretase inhibitor	NOTCH1 | PSEN1	Non-epigenetic	Non-epigenetic
Rocilinostat	53340666	Phase 1/Phase 2	Ricolinostat (ACY-1215) is a potent and selective HDAC6 inhibitor, with an IC50 of 5 nM. ACY-1215 also inhibits HDAC1, HDAC2, and HDAC3 with IC50s of 58, 48, and 51 nM, respectively	hdac inhibitor	HDAC1 | HDAC2 | HDAC3 | HDAC6 | HDAC8	Eraser	HDACi
Rosiglitazone	77999	Withdrawn	Antihyperglycemic agent and a potent thiazolidinedione insulin sensitizer with IC50 of 12, 4 and 9 nM for rat, 3T3-L1 and human adipocytes, respectively	insulin sensitizer | insulin sensitizer, ppar receptor agonist | ppar receptor agonist	CYP2C8 | FFAR1 | INS | PPARG | TRPC5 | TRPM3	Non-epigenetic	Non-epigenetic
Rosuvastatin	446157	Launched	Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.	hmgcr inhibitor	HMGCR	Non-epigenetic	Non-epigenetic
RS 17053 hydrochloride	9824953	Preclinical	RS 17053 hydrochloride is a potent and selective α1A adrenoceptor antagonist, with a pKi value of 9.1 in native cell membrane and a pA2 value of 9.8 in functional assays	adrenergic receptor antagonist	ADRA1A | ADRA1D	Non-epigenetic	Non-epigenetic
Rucaparib	9931954	Phase 3	Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research	parp inhibitor	PARP1 | PARP2	Non-epigenetic	Non-epigenetic
Ruxolitinib	25126798	Launched	Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3. Ruxolitinib kills tumor cells through toxic mitophagy. Ruxolitinib induces autophagy and enhances apoptosis	jak inhibitor	JAK1 | JAK2 | JAK3 | TYK2	Non-epigenetic	Non-epigenetic
Ruxolitinib + Paclitaxel		Launched | Launched	Combination: Ruxolitinib + Paclitaxel	jak inhibitor | tubulin polymerization inhibitor	ABCB1 | BCL2 | CYP2C8 | JAK1 | JAK2 | JAK3 | MAP2 | MAP4 | MAPT | NR1I2 | TLR4 | TUBA1A | TUBA1B | TUBA1C | TUBA3C | TUBA3D | TUBA3E | TUBA4A | TUBB | TUBB1 | TUBB2A | TUBB2B | TUBB3 | TUBB4A | TUBB4B | TUBB6 | TUBB8 | TYK2	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Ryuvidine	481747	Preclinical	Ryuvidine is a potent inhibitor of SET domain-containing protein 8(SETD8) with an IC50 of 0.5 µM and suppresses monomethylation of H4K20 in vitro. Ryuvidine also inhibits CDK4 with an IC50 of 6.0 μM and is cytotoxic against a range of human cancer cells	histone lysine methyltransferase inhibitor	CDK2 | CDK4	Writer	HMTi
S2101	121513887	Preclinical	Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 0.99 μM, Ki of 0.61 μM and Kinact/Ki of 4560 M/s.	histone lysine demethylase inhibitor	KDM1A	Eraser	HDMi
Samotolisib	57519748	Phase 2	Samotolisib (LY3023414) potently and selectively inhibits class I PI3K isoforms, DNA-PK, and mTORC1/2 with IC50s of 6.07 nM, 77.6 nM, 38 nM, 23.8 nM, 4.24 nM and 165 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ, DNA-PK and mTOR, respectively. Samotolisib potently inhibits mTORC1/2 at low nanomolar concentrations	mtor inhibitor | pi3k inhibitor	AKT1 | MTOR	Non-epigenetic	Non-epigenetic
Sanguinarine chloride	68635	Preclinical	Sanguinarine (Sanguinarin) chloride, a benzophenanthridine alkaloid derived from the root of Sanguinaria Canadensis, can stimulate apoptosis via activating the production of reactive oxygen species (ROS). Sanguinarine-induced apoptosis is associated with the activation of JNK and NF-κB.	apoptosis stimulant	JNK | NFKB	Non-epigenetic	Non-epigenetic
Saracatinib	10302451	Phase 2/Phase 3	Saracatinib (AZD0530) is a potent Src inhibitor with IC50 of 2.7 nM in cell-free assays, and potent to c-Yes, Fyn, Lyn, Blk, Fgr and Lck; less active for Abl and EGFR (L858R and L861Q). Saracatinib induces autophagy. Phase 2/3	src inhibitor	ABL1 | LCK | SRC | YES1	Non-epigenetic	Non-epigenetic
Saridegib	25027363	Preclinical	Saridegib is a potent and specific inhibitor of Smoothened (Smo), a key signaling transmembrane protein in the Hedgehog (Hh) pathway	smoothened receptor inhibitor	SMO	Non-epigenetic	Non-epigenetic
Satraplatin	6918220	Phase 3	Satraplatin is an alkylating agent, with potent antitumor effect	dna alkylating agent	DNA	Non-epigenetic	Non-epigenetic
Savolitinib	68289010	Phase 3	Volitinib is an orally bioavailable inhibitor of the c-Met receptor tyrosine kinase with potential antineoplastic activity	c-met inhibitor	MET	Non-epigenetic	Non-epigenetic
SB 216641 hydrochloride	10392025	Preclinical	SB-216641A (SB-216641 hydrochloride) is a selective antagonist of 5-HT1B/D receptor. SB-216641A shows high affinity and selectivity for h5-HT1B receptors over h5-HT1D receptors. SB-216641A inhibits the function of SKF-99101H	serotonin receptor antagonist	HTR1A | HTR1B | HTR1D | HTR2A | HTR2B | HTR2C	Non-epigenetic	Non-epigenetic
SB-225002	3854666	Preclinical	CXCR2 antagonist with IC50 of 22 nM for inhibiting interleukin IL-8 binding to CXCR2, >150-fold selectivity over the other 7-TMRs tested.	cc chemokine receptor antagonist	CXCR2	Non-epigenetic	Non-epigenetic
SB-743921	9936388	Phase 1/Phase 2	Kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, almost no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E. Phase 1/2	kinesin-like spindle protein inhibitor	KIF11	Non-epigenetic	Non-epigenetic
SBI-756	121241171	Preclinical	SBI-0640756 (SBI-756) is an inhibitor of eIF4G1 and disrupts the eIF4F complex.	eif4g1 inhibitor	EIF4G1	Non-epigenetic	Non-epigenetic
SCH-529074	12001922	Preclinical	SCH529074 is a potent and orally active p53 activator. SCH529074 binds specifically and conformation-dependently to p53 DBD ( DNA binding domain) with a Ki of 1-2 μM in a saturable manner. SCH529074 restores mutant p53 function and interrupts HDM2-mediated ubiquitination of wild Type p53. SCH529074 can be used for the study of non-small-cell lung carcinoma (NSCLC).	p53 activator	TP53	Non-epigenetic	Non-epigenetic
SCH-79797	4259181	Preclinical	SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.	parp antagonist	PARP1	Non-epigenetic	Non-epigenetic
Scriptaid	5186	Preclinical	Scriptaid is a potent histone deacetylase (HDAC) inhibitor, used in cancer research. Scriptaid is also a sensitizer to antivirals and has potential for epstein-barr virus (EBV)-associated lymphomas treatment	hdac inhibitor	HDAC1 | HDAC2 | HDAC3 | HDAC4 | HDAC5 | HDAC6 | HDAC7 | HDAC8 | HDAC9	Eraser	HDACi
Selinexor	71481097	Launched	Selinexor (KPT-330), analog of KPT-185, is an orally bioavailable and selective CRM1 inhibitor	exportin antagonist	XPO1	Non-epigenetic	Non-epigenetic
Selumetinib	10127622	Phase 3	Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation	mek inhibitor	MAP2K1 | MAP2K2	Non-epigenetic	Non-epigenetic
Serdemetan	11609586	Phase 1	Serdemetan(JNJ-26854165) acts as a HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53	mdm inhibitor	MDM2	Non-epigenetic	Non-epigenetic
SGC-CBP30	72201027	Preclinical	CBP/EP300 Bromodomain inhibition	bromodomain inhibitor	CREBBP | EP300	Reader | Writer	HATi | PAHi
SGI-1776 free base	24795070	Phase 1	SGI-1776 free base is an inhibitor of Pim kinases, with IC50s of 7 nM, 363 nM, and 69 nM for Pim-1, -2 and -3, respectively	pim kinase inhibitor	FLT3 | PIM1 | PIM2 | PIM3	Non-epigenetic	Non-epigenetic
shBRD2		N/A	BRD2 knockdown	short hairpin rna	BRD2	Reader	PAHi
shBRD3		N/A	BRD3 knockdown	short hairpin rna	BRD3	Reader	PAHi
shBRD4		N/A	BRD4 knockdown	short hairpin rna	BRD4	Reader	PAHi
shBRM		N/A		short hairpin rna	BRM	Non-epigenetic	Non-epigenetic
shIGF2BP1		N/A	Selinexor (KPT-330, ATG-010) is an orally bioavailable selective CRM1 inhibitor. Phase 2	short hairpin rna	IGF2BP1	Non-epigenetic	Non-epigenetic
shMETTl14		N/A	HDM2 ubiquitin ligase antagonist and also induces early apoptosis in p53 wild-type cells, inhibits cellular proliferation followed by delayed apoptosis in the absence of functional p53. Phase 1	short hairpin rna	METTL14	Non-epigenetic	Non-epigenetic
shRen.713		N/A		short hairpin rna		Non-epigenetic	Non-epigenetic
shRNA BRD4		N/A	BRD4 Knockdown	short hairpin rna	BRD4	Reader	PAHi
shSETD2		N/A	BRD4 Knockdown	short hairpin rna	SETD2	Writer	HMTi
siBEGAIN		N/A	BEGAIN knockdown	small interfering rna	BEGAIN	Non-epigenetic	Non-epigenetic
siBRD4		N/A	Combination: BRD4 si + Heat Shock Treatment	small interfering rna	BRD4	Reader	PAHi
siBRD4 + Heat Shock Treatment		N/A	Combination: BRD4 si + Heat Shock Treatment	small interfering rna	BRD4	Reader | Non-epigenetic	PAHi | Non-epigenetic
siCCNK		N/A	CCNK knockdown	small interfering rna	CCNK	Non-epigenetic	Non-epigenetic
siCDH4		N/A	Cadherin-4 inhibitor	small interfering rna	CADHERIN-4	Non-epigenetic	Non-epigenetic
siCDK10		N/A	CDK10 knockdown	small interfering rna	CDK10	Non-epigenetic	Non-epigenetic
siCREM		N/A	CREM knockdown	small interfering rna	CREM	Non-epigenetic	Non-epigenetic
siCTNNB1		N/A	Beta-Catenin inhibitor	small interfering rna	BETA-CATENIN	Non-epigenetic	Non-epigenetic
siCTR		N/A	CTR knockdown	small interfering rna	Control	Non-epigenetic	Non-epigenetic
siDMNT1		N/A	DNA Methyltransferase 1 inhibitor	small interfering rna	DNMT1	Writer	DNMTi
siDMNT1 + siCDH4		N/A	Combination: DNA Methyltransferase 1 inhibitor and Cadherin-4 inhibitor	small interfering rna	DNMT1 | CADHERIN-4	Writer | Non-epigenetic	DNMTi | Non-epigenetic
siDPPA5		N/A	DPPA5 knockdown	small interfering rna	DPPA5	Non-epigenetic	Non-epigenetic
siEIF3L		N/A	EIF3L knockdown	small interfering rna	EIF3L	Non-epigenetic	Non-epigenetic
siFUBP1		N/A	FUBP1 knockdown	small interfering rna	FUBP1	Non-epigenetic	Non-epigenetic
siGLI1		N/A	GLI1 knockdown	small interfering rna	GLI1	Non-epigenetic	Non-epigenetic
siHMGCR		N/A	siRNA_si104864	small interfering rna	HMG-CoA reductase	Non-epigenetic	Non-epigenetic
siHuR		N/A	HuR knockdown	small interfering rna	HuR	Non-epigenetic	Non-epigenetic
siJAK2		N/A	JAK2 knockdown	small interfering rna	JAK2	Non-epigenetic	Non-epigenetic
Simvastatin	54454	Launched	Simvastatin (MK 733) is a competitive inhibitor of HMG-CoA reductase with a Ki of 0.2 nM.	hmgcr inhibitor	CYP2C8 | CYP3A4 | CYP3A5 | HMGCR | ITGB2	Non-epigenetic	Non-epigenetic
siNeg		N/A	siRNA DNA Methyltransferase 1 knockdown	small interfering rna		Non-epigenetic	Non-epigenetic
siNFYA		N/A	NFYA knockdown	small interfering rna	NFYA	Non-epigenetic	Non-epigenetic
siP4HB + siPDIA1		N/A	Combination: siP4HB + siPDIA1	small interfering rna	P4HB, PDIA1	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
siPOLR2D		N/A	POLR2D knockdown	small interfering rna	POLR2D	Non-epigenetic	Non-epigenetic
siPSMD13		N/A	PSMD13 knockdown	small interfering rna	PSMD13	Non-epigenetic	Non-epigenetic
siRBM3		N/A	RBM3 knockdown	small interfering rna	RBM3	Non-epigenetic	Non-epigenetic
siRGS18		N/A	RGS18 knockdown	small interfering rna	RGS18	Non-epigenetic	Non-epigenetic
siRNA		N/A	siRNA targeting of E2 reversed repression of HPV16 E2 targeted genes	small interfering rna		Non-epigenetic	Non-epigenetic
siRNA + GapmeR		N/A	siRNA + GapmeR	small interfering rna		Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
siSAP130		N/A	SAP130 knockdown	small interfering rna	SAP130	Non-epigenetic	Non-epigenetic
siTGM5		N/A	TGM5 knockdown	small interfering rna	TGM5	Non-epigenetic	Non-epigenetic
siTOX4		N/A	TOX4 knockdown	small interfering rna	TOX4	Non-epigenetic	Non-epigenetic
siZC3H14		N/A	ZC3H14 knockdown	small interfering rna	ZC3H14	Non-epigenetic	Non-epigenetic
siZFC3H1		N/A	ZFC3H1 knockdown	small interfering rna	ZFC3H1	Non-epigenetic	Non-epigenetic
SN-38	104842	Launched	SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively	topoisomerase inhibitor	TOP1	Non-epigenetic	Non-epigenetic
SNAP 5089	56972175	Preclinical	SNAP 5089 is a subtype-selective α1A-adrenoceptor antagonist that displays > 600-fold selectivity over other adrenoceptors (Kivalues are 0.35, 220, 370, 540, 800 and 1200 nM for α1A, α1B, α2C, α1D, α2B and α2A subtypes respectively and 540 nM for L-type Ca2+ channels). Inhibits noradrenalin-induced contractions in rabbit vascular and lower urinary tissues	adrenergic receptor antagonist	ADRA1A | ADRA1B | ADRA1D | ADRA2A | ADRA2B | ADRA2C | CACNA1C | CACNA1D	Non-epigenetic	Non-epigenetic
SNX-2112	24772860	Phase 1	Selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30nM, uniformly more potent than 17-AAG	hsp inhibitor		Non-epigenetic	Non-epigenetic
Sodium Butyrate	5222465	Preclinical	Sodium Butyrate is the sodium salt of butyrate with potential antineoplastic activity. Butyrate, a short chain fatty acid, competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). This binding affects hyperacetylation of histones, resulting in a modified DNA conformation, which subsequently leads to the uncoiling or relaxing of chromatin. Enhanced accessibility of chromatin to transcription-regulatory complexes leads to increased transcriptional activation of various epigenetically suppressed genes. Butyrate, a HDAC inhibitor, induces cell cycle arrest in G1 or G2/M and also increases the expression of other genes and proteins involved in cellular differentiation and apoptotic signaling.	hdac inhibitor	CYP3A5 | HDAC1	Eraser	HDACi
Sonidegib	24775005	Launched	Sonidegib (Erismodegib) is a potent and selective Smo antagonist with IC50 of 1.3 nM and 2.5 nM for mouse and human Smo in binding assay, respectively	smoothened receptor antagonist	SMO	Non-epigenetic	Non-epigenetic
Sorafenib	216239	Launched	Multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90nM, respectively.	flt3 inhibitor | kit inhibitor | pdgfr tyrosine kinase receptor inhibitor | raf inhibitor | ret tyrosine kinase inhibitor | vegfr inhibitor	BRAF | CYP2B6 | CYP2C8 | CYP3A5 | DDR2 | FGFR1 | FLT1 | FLT3 | FLT4 | KDR | KIT | PDGFB | PDGFRB | RAF1 | RET | SLCO1B3	Non-epigenetic	Non-epigenetic
Sotrastaurin	10296883	Phase 2	Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively	pkc inhibitor	PRKCA | PRKCB | PRKCD | PRKCE | PRKCH | PRKCQ	Non-epigenetic	Non-epigenetic
sPDL1		N/A	Soluble PDl-1	N/A		Non-epigenetic	Non-epigenetic
SR 33805 oxalate	21256218	Preclinical	SR33805 oxalate is a potent Ca2+ channel antagonist, with EC50s of 4.1 nM and 33 nM in depolarized and polarized conditions, respectively. SR33805 oxalate blocks L-type but not T-type Ca2+ channels. SR33805 oxalate can be used for the research of acute or chronic failing hearts.	calcium channel antagonist	CACNA2D2	Non-epigenetic	Non-epigenetic
SRT1720	25232708	Preclinical	SRT 1720 is a selective activator of human SIRT1 with an EC1.5 of 0.16 μM, and shows less potent activities for SIRT2 and SIRT3 with EC1.5s of 37 μM and > 300 μM, respectively	sirt activator	SIRT1	Eraser	HDACi
Stattic	2779853	Preclinical	Stattic is a potent STAT3 inhibitor and inhibits STAT3 phosphorylation (at Y705 and S727). Stattic inhibits the binding of a high affinity phosphopeptide for the SH2 domain of STAT3. Stattic ameliorates the renal dysfunction in Alport syndrome (AS) mice	stat inhibitor	STAT3	Non-epigenetic	Non-epigenetic
SU11274	9549297	Preclinical	Met inhibitor with IC50 of 10 nM, no effects on PGDFRβ, EGFR or Tie2.	hepatocyte growth factor receptor inhibitor | tyrosine kinase inhibitor	MET	Non-epigenetic	Non-epigenetic
Suberanilohydroxamic Acid	5311	Launched	SAHA has KLF2-dependent anti-inflammatory effects in endothelial cells	hdac inhibitor	HDAC1 | HDAC10 | HDAC11 | HDAC2 | HDAC3 | HDAC5 | HDAC6 | HDAC8 | HDAC9	Eraser	HDACi
Sudemycin D6	74762666	Preclinical	Proprietary small-molecule splicing modulator that targets splicing factor 3B subunit 1 (SF3B1)	rna splicing modifier	DUSP11 | SRMM11	Non-epigenetic	Non-epigenetic
Sunitinib	5329102	Launched	Multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80nM and 2 nM, and also inhibits c-Kit	flt3 inhibitor | kit inhibitor | pdgfr tyrosine kinase receptor inhibitor | ret tyrosine kinase inhibitor | vegfr inhibitor	CSF1R | FGFR1 | FLT1 | FLT3 | FLT4 | KDR | KIT | PDGFRA | PDGFRB | RET	Non-epigenetic	Non-epigenetic
SY0351		Preclinical	SY0351 a THZ1-based inhibitor with improved selectivity towards CDK7 showed efficient antitumor effects in multiple AML xenograft models and extended previous views of CDK7 as a direct activator for the CDK-activating kinase for CDKs9/12 and 13	cdk inhibitor	CDK7	Non-epigenetic	Non-epigenetic
Tacedinaline	2746	Phase 3	Tacedinaline (N-acetyldinaline) is an inhibitor of the histone deacetylase (HDAC) with IC50s of 0.9, 0.9, 1.2 μM for recombinant HDAC 1, 2 and 3 respectively	hdac inhibitor	HDAC1	Eraser	HDACi
Tacrolimus	445643	Launched	Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties	calcineurin inhibitor	CYP3A5 | CYP3A7 | FKBP1A	Non-epigenetic	Non-epigenetic
TAK733	24963252	Phase 1	TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM	mek inhibitor	MAP2K1	Non-epigenetic	Non-epigenetic
Talampanel	164509	Phase 2	Talampanel (LY300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity. Talampanel (IVAX) has neuroprotective effects in rodent stroke models. Talampanel attenuates caspase-3 dependent apoptosis in mouse brain	glutamate receptor antagonist	GRIA1 | GRIA2 | GRIA3 | GRIA4	Non-epigenetic	Non-epigenetic
Talazoparib	135565082	Launched	Talazoparib (BMN-673) is a highly potent, orally active PARP1/2 inhibitor.Talazoparib inhibits PARP1 and PARP2 enzyme activity with Kis of 1.2 nM and 0.87 nM, respectively. Talazoparib has antitumor activity	parp inhibitor	PARP1 | PARP2	Non-epigenetic	Non-epigenetic
Talmapimod	9871074	Phase 2	Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs	p38 mapk inhibitor	IL1B | MAPK11 | MAPK14 | MT-CO2 | TNF	Non-epigenetic	Non-epigenetic
Tamoxifen	2733526	Launched	Tamoxifen (ICI 47699) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.	estrogen receptor antagonist | selective estrogen receptor modulator (serm)	CYP3A5 | EBP | ESR1 | ESR2 | GPER1 | PRKCA | PRKCB | PRKCD | PRKCE | PRKCG | PRKCI | PRKCQ | PRKCZ	Non-epigenetic	Non-epigenetic
Tandutinib	3038522	Phase 2	Tandutinib (MLN518) is a potent and selective inhibitor of the FLT3 with an IC50 of 0.22 μM, and also inhibits c-Kit and PDGFR with IC50s of 0.17 μM and 0.20 μM, respectively. Tandutinib can be used for acute myelogenous leukemia (AML). Tandutinib has the ability to cross the blood-brain barrier	flt3 inhibitor | kit inhibitor | pdgfr tyrosine kinase receptor inhibitor	CSF1R | FLT3 | KIT | PDGFD | PDGFRA | PDGFRB	Non-epigenetic	Non-epigenetic
Tariquidar	148201	Phase 3	Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM)	p glycoprotein inhibitor	ABCB1	Non-epigenetic	Non-epigenetic
Tasisulam	10160238	Phase 3	Tasisulam is a anticancer agent and induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death. Tasisulam inhibits mitotic progression and induces vascular normalization	apoptosis stimulant		Non-epigenetic	Non-epigenetic
Tasquinimod	54682876	Phase 3	Tasquinimod is an oral antiangiogenic agent, which has the potential for castration-resistant prostate cancer treatment. Tasquinimod binds to the regulatory Zn2+ binding domain of HDAC4 with Kd of 10-30 nM. Tasquinimod also is a S100A9 inhibitor	angiogenesis inhibitor | s100a9 inhibitor	HDAC4 | S100A9	Eraser | Non-epigenetic	HDACi | Non-epigenetic
Tazemetostat	66558664	Launched	Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a Ki value of 2.5 nM. Tazemetostat (EPZ-6438) inhibits EZH2 with IC50s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat (EPZ-6438) inhibits rat EZH2 with an IC50 of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC50 of 392 nM.	histone lysine methyltransferase inhibitor	EZH2	Writer	HMTi
Tedizolid	11234049	Launched	Novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome	bacterial 50s ribosomal subunit inhibitor		Non-epigenetic	Non-epigenetic
Telatinib	9808844	Phase 2	Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively	kit inhibitor | pdgfr tyrosine kinase receptor inhibitor | vegfr inhibitor	FLT4 | KDR | KIT | PDGFRB	Non-epigenetic	Non-epigenetic
Temozolomide	5394	Launched	Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects	dna alkylating agent	MGMT | TOP2A	Non-epigenetic	Non-epigenetic
Temozolomide + Olaparib		Launched | Launched	Combination: Temozolomide + Olaparib	dna alkylating agent | parp inhibitor	MGMT | PARP1 | PARP2 | PARP3 | TOP2A	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Temsirolimus	6918289	Launched	Temsirolimus is an inhibitor of mTOR with an IC50 of 1.76 μM. Temsirolimus activates autophagy and prevents deterioration of cardiac function in animal model	mtor inhibitor	MTOR | PTEN	Non-epigenetic	Non-epigenetic
Teniposide	452548	Launched	Teniposide is a semisynthetic derivative of podophyllotoxin that exhibits antitumor activity. Teniposide inhibits DNA synthesis by forming a complex with topoisomerase II and DNA. This complex induces breaks in double stranded DNA and prevents repair by topoisomerase II binding. Accumulated breaks in DNA prevent cells from entering into the mitotic phase of the cell cycle, and lead to cell death. Teniposide acts primarily in the G2 and S phases of the cycle.	topoisomerase inhibitor	CYP3A5 | TOP2A | TOP2B	Non-epigenetic	Non-epigenetic
Tepoxalin	59757	Launched	Tepoxalin is a nonsteroidal anti-inflammatory drug approved for veterinary use in the United States and many other countries. It is primarily used to reduce inflammation and relief of pain caused by musculoskeletal disorders such as hip dysplasia and arthritis.	cyclooxygenase inhibitor | lipoxygenase inhibitor	ALOX5	Non-epigenetic	Non-epigenetic
Terfenadine	5405	Withdrawn	Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9	histamine receptor antagonist	HRH1 | KCNH1 | KCNH2	Non-epigenetic	Non-epigenetic
Tet Off		N/A	Dominant-negative CDK9 (dnCDK9) overexpression (tetOff)	cdk regulator	CDK9	Non-epigenetic	Non-epigenetic
Tetrindole mesylate	54792409	Phase 3	Tetrindole mesylate is a selective inhibitor of monoamine oxidase A (MAO A). Tetrindole mesylate inhibits rat brain mitochondrial MAO A in a competitive manner with a Ki value of 0.4 μM and inhibits MAO B with a Ki of 110 μM. Tetrindole mesylate has antidepressant activity	monoamine oxidase inhibitor	MAOA	Non-epigenetic	Non-epigenetic
TG003	1893668	Preclinical	TG003 is a potent inhibitor of Clk1/Sty; inhibits Clk1 and Clk4 with IC50 values of 20 and 15 nM, respectively	clk inhibitor	CLK1 | CLK4 | DYRK1A | DYRK1B	Non-epigenetic	Non-epigenetic
TGF alpha		N/A	Transforming growth factor-alpha	growth factor receptor inhibitor	TGFA	Non-epigenetic	Non-epigenetic
TGFβ		N/A	Transforming growth factor-beta	growth factor receptor inhibitor	TGFB	Non-epigenetic	Non-epigenetic
TGFβ + Nutlin 3		N/A | Preclinical	Combination: Transforming growth factor-Œ≤ and (Nutlin 3) Mdm2 (RING finger-dependent ubiquitin protein ligase for itself and p53) antagonist with IC50 of 90 nM in a cell-free assay; stabilizes p73 in p53-deficient cells.	growth factor receptor inhibitor | mdm inhibitor	MDM2 | TGFB | TP53	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Thalidomide	5426	Launched	Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate	tumor necrosis factor production inhibitor	CRBN | CYP1A2 | CYP2B6 | CYP2C19 | CYP3A5 | TNF	Non-epigenetic	Non-epigenetic
Thapsigargin	446378	Preclinical	Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca2+-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types.	endoplasmic reticulum stress inducer		Non-epigenetic	Non-epigenetic
Thioguanine	2723601	Launched	6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively	purine antagonist	IMPDH1 | IMPDH2	Non-epigenetic	Non-epigenetic
Thiotepa	5453	Launched	Thio-TEPA is a DNA alkylating agent, with antitumor activity	cytochrome p450 inhibitor	CYP2B6 | CYP3A4	Non-epigenetic	Non-epigenetic
THZ1	73602827	Preclinical	Selective and potent covalent CDK7 inhibitor with an IC50 of 3.2 nM. THZ1 also inhibits the closely related kinases CDK12 and CDK13 and downregulates MYC expression	cdk inhibitor	CDK7	Non-epigenetic	Non-epigenetic
THZ1 + I-BET151		Preclinical | Preclinical	Combination: THZ1 + I-BET151	bromodomain inhibitor | cdk inhibitor	BRD2 | BRD3 | BRD4 | CDK7	Reader | Non-epigenetic	PAHi | Non-epigenetic
THZ531	118025540	Preclinical	THZ531 is a selective and covalent inhibitor of both CDK12 and CDK13 with IC50s of 158 nM and 69 nM, respectively.	cdk inhibitor	CDK12 | CDK13	Non-epigenetic	Non-epigenetic
Tirabrutinib	54755438	Launched	Tirabrutinib (ONO-4059) is an orally active Bruton’s Tyrosine Kinase (BTK) inhibitor (can cross the blood-brain barrier (BBB)), with an IC50 of 6.8 nM. Tirabrutinib irreversibly and covalently binds to BTK and inhibits aberrant B cell receptor signaling. Tirabrutinib can be used in studies of autoimmune diseases and hematological malignancies.	bruton's tyrosine kinase (btk) inhibitor	BTK	Non-epigenetic	Non-epigenetic
Tirapazamine	135413511	Phase 3	Tirapazamine (SR259075) is an anticancer agent that shows selective cytotoxicity for hypoxic cells in solid tumors, thereby inducing single-and double-strand breaks in DNA, base damage, and cell death. Tirapazamine is an anticancer and bioreductive agent.Tirapazamine (SR259075) can enhance the cytotoxic effects of ionizing radiation in hypoxic cells	dna inhibitor		Non-epigenetic	Non-epigenetic
Tivantinib	11494412	Phase 3	Non-ATP-competitive c-Met inhibitor with Ki of 0.355μM in a cell-free assay, little activity to Ron, and no inhibition to EGFR, InsR, PDGFRα or FGFR1/4. Phase 3.	tyrosine kinase inhibitor	MET	Non-epigenetic	Non-epigenetic
Tivozanib	9911830	Launched	Tivozanib (AV-951; KRN951) is a selective, orally active inhibitor for vascular endothelial growth factor receptor (VEGFR)-1, 2 3, with IC50s of 30, 6.5 and 15 nM, respectively. Tivozanib exhibits antitumor efficacy	vegfr inhibitor	FLT1 | FLT4 | KDR | KIT | PDGFRA | PDGFRB	Non-epigenetic	Non-epigenetic
TLP-KD		N/A	TLP knockdown	tlp regulator	TLP	Non-epigenetic	Non-epigenetic
TNFa		N/A	Tumor necrosis factor alpha	tumor necrosis factor production inhibitor		Non-epigenetic	Non-epigenetic
TNFa + siRNA + GapmeR		N/A	Combination: (TNFa) (siRNA) and (GapmeR)	tumor necrosis factor production inhibitor		Non-epigenetic | Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Tofacitinib	9926791	Launched	Tofacitinib is an orally available JAK3/2/1 inhibitor with IC50s of 1, 20, and 112 nM, respectively	jak inhibitor	CYP2C19 | JAK1 | JAK2 | JAK3	Non-epigenetic	Non-epigenetic
Topotecan	60700	Launched	Topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells withIC50of 13 nM and 2 nM, respectively	topoisomerase inhibitor	TOP1 | TOP1MT	Non-epigenetic	Non-epigenetic
Toremifene	3005573	Launched	Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively	estrogen receptor antagonist | selective estrogen receptor modulator (serm)	CYP3A5 | ESR1	Non-epigenetic	Non-epigenetic
Torin1	49836027	Preclinical	Torin 1 is a potent inhibitor of mTOR with an IC50 of 3 nM. Torin 1 inhibits both mTORC1/2 complexes with IC50 values between 2 and 10 nM. Torin 1 is an effective inducer of autophagy	mtor inhibitor	MTOR | PIK3CA	Non-epigenetic	Non-epigenetic
Tovorafenib	25161177	Phase 1/Phase 2	Tovorafenib (TAK-580, MLN 2480) is an orally active and selective inhibitor of pan-Raf kinase	raf inhibitor		Non-epigenetic	Non-epigenetic
Trametinib	11707110	Launched	Trametinib (GSK1120212; JTP-74057) is an orally active MEK inhibitor that inhibits MEK1 and MEK2 with IC50s of about 2 nM. Trametinib activates autophagy and induces apoptosis.	mek inhibitor	CYP2C8 | CYP3A4 | MAP2K1 | MAP2K2	Non-epigenetic	Non-epigenetic
Trametinib + I-BET151		Launched | Preclinical	Combination: Trametinib + IBET151	bromodomain inhibitor | mek inhibitor	BRD2 | BRD3 | BRD4 | CYP2C8 | CYP3A4 | MAP2K1 | MAP2K2	Reader | Writer	HATi | PAHi
Trametinib + JQ1		Launched | Preclinical	Combination: Trametinib + JQ1	bromodomain inhibitor | mek inhibitor	BRD2 | BRD3 | BRD4 | BRDT | CYP2C8 | CYP3A4 | MAP2K1 | MAP2K2	Reader | Writer	HATi | PAHi
Trametinib + SGC-CBP30		Launched | Preclinical	Combination: Trametinib + SGCCBP30	bromodomain inhibitor | mek inhibitor	CREBBP | CYP2C8 | CYP3A4 | EP300 | MAP2K1 | MAP2K2	Reader | Writer	HATi | PAHi
Tretinoin	444795	Launched	Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha	retinoid receptor agonist | retinoid receptor ligand	ALDH1A1 | ALDH1A2 | GPRC5A | NR0B1 | NR2C2 | PPARD | RARA | RARB | RARG | RARRES1 | RORB | RORC | RXRB | RXRG	Non-epigenetic	Non-epigenetic
Triamterene	5546	Launched	Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic. Triamterene as an inhibitor of the TGR5 receptor.	sodium channel blocker	SCNN1A | SCNN1B | SCNN1D | SCNN1G	Non-epigenetic	Non-epigenetic
Triapine	9571836	Phase 2	Triapine (3-AP; PAN-811) is a potent inhibitor of the M2 subunit of ribonucleotide reductase (RR), and is a potent radiosensitizer	ribonucleotide reductase inhibitor	RRM1 | RRM2	Non-epigenetic	Non-epigenetic
Trichostatin A	444732	Phase 1	Potent and specific inhibitor of HDAC class I/II, with an IC50 value of 1.8 nM for HDAC.	hdac inhibitor	HDAC1 | HDAC10 | HDAC2 | HDAC3 | HDAC4 | HDAC5 | HDAC6 | HDAC7 | HDAC8 | HDAC9	Eraser	HDACi
Triciribine	65399	Phase 1/Phase 2	Triciribine is a DNA synthesis inhibitor, also inhibits Akt and HIV-1/2 with IC50 of 130 nM, and 0.02-0.46 μM, respectively	akt inhibitor	AKT1 | AKT2 | AKT3	Non-epigenetic	Non-epigenetic
Trifluridine	6256	Launched	Trifluridine (Trifluorothymidine) is an irreversible and orally active thymidylate synthase inhibitor, and thereby suppressing DNA synthesis. Trifluridine is an antiviral molecule used for research of HSV, rhabdovirus and orthopoxvirus infection. Trifluridine induces cell apoptosis and autophagy. Trifluridine is also an anticancer agent used in studies of metastatic colorectal cancer, gastrointestinal tumors	dna directed dna polymerase inhibitor | thymidylate synthase inhibitor	TYMS	Non-epigenetic	Non-epigenetic
Triptolide	107985	Phase 3	Triptolide is a diterpenoid triepoxide extracted from the root of Tripterygium wilfordii with immunosuppressive, anti-inflammatory, antiproliferative and antitumour effects. Triptolide is a NF-κB activation inhibitor.	rna polymerase inhibitor	CYP2C19 | RELA	Non-epigenetic	Non-epigenetic
TW-37	11455910	Preclinical	Nonpeptide inhibitor to recombinant Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.29μM, 1.11μM and 0.26μM, respectively	bcl inhibitor	BCL2 | BCL2L1 | MCL1	Non-epigenetic	Non-epigenetic
UCN01	72271	Phase 2	PKC inhibitor	cdk inhibitor | chk inhibitor | pkc inhibitor	AKT1 | CDK1 | CDK2 | CDK4 | CDK6 | CHEK1 | CHEK2 | GSK3B | LCK | MAPK14 | MARK1 | MARK3 | PDPK1 | PRKCA | PRKCB | PRKCD | PRKCE | PRKCG	Non-epigenetic	Non-epigenetic
UNC0638	46224516	Preclinical	UNC0638 selectively inhibits G9a and GLP histone methyltransferase activity with IC50s of less than 15 nM and 19 nM, respectively. UNC0638 has anti-FMDV (foot-and-mouth disease virus) and anti-VSV (vesicular stomatitis virus) activities	histone lysine methyltransferase inhibitor	EHMT1 | EHMT2	Writer	HMTi
Vadimezan	123964	Phase 3	Vadimezan (DMXAA; ASA-404), the tumor vascular disrupting agent (tumor-VDA), is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines. Vadimezan has anti-influenza virus H1N1-PR8 activities	angiogenesis inhibitor		Non-epigenetic	Non-epigenetic
Valproic Acid	3121	Launched	Valproic acid (VPA) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid is used in the treatment of epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches	benzodiazepine receptor agonist | hdac inhibitor	ABAT | ACADSB | ALDH5A1 | HDAC1 | HDAC2 | HDAC9 | OGDH | SCN10A | SCN11A | SCN1A | SCN1B | SCN2A | SCN2B | SCN3A | SCN3B | SCN4A | SCN4B | SCN5A | SCN7A | SCN8A | SCN9A	Eraser | Non-epigenetic	HDACi | Non-epigenetic
Valproic Acid + IFNy		Launched	Combination: Valproic Acid + IFNy	benzodiazepine receptor agonist | hdac inhibitor	ABAT | ACADSB | ALDH5A1 | HDAC1 | HDAC2 | HDAC9 | OGDH | SCN10A | SCN11A | SCN1A | SCN1B | SCN2A | SCN2B | SCN3A | SCN3B | SCN4A | SCN4B | SCN5A | SCN7A | SCN8A | SCN9A	Eraser | Non-epigenetic	HDACi | Non-epigenetic
Vandetanib	3081361	Launched	Vandetanib (D6474) is a potent, orally active inhibitor of VEGFR2/KDR tyrosine kinase activity (IC50=40 nM). Vandetanib also has activity versus the tyrosine kinase activity of VEGFR3/FLT4 (IC50=110 nM) and EGFR/HER1 (IC50=500 nM)	egfr inhibitor | ret tyrosine kinase inhibitor | vegfr inhibitor	EGFR | EPHA1 | EPHA10 | EPHA2 | EPHA3 | EPHA4 | EPHA5 | EPHA6 | EPHA7 | EPHA8 | EPHB1 | EPHB2 | EPHB3 | EPHB4 | EPHB6 | ERBB2 | ERBB3 | ERBB4 | FLT1 | FLT3 | FLT4 | KDR | KIT | PTK6 | RET | SRC | TEK | VEGFA	Non-epigenetic	Non-epigenetic
Varlitinib	42642648	Phase 2/Phase 3	Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively	egfr inhibitor	EGFR | ERBB2 | ERBB4	Non-epigenetic	Non-epigenetic
Vatalanib	151194	Phase 3	Vatalanib (PTK787; ZK-222584; CGP-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM	kit inhibitor | pdgfr tyrosine kinase receptor inhibitor | vegfr inhibitor	CYP19A1 | EGFR | FLT1 | FLT4 | KDR | KIT | PDGFRA | PDGFRB	Non-epigenetic	Non-epigenetic
Vemurafenib	42611257	Launched	Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.	raf inhibitor	BRAF | CYP2C19 | CYP3A4 | CYP3A5 | RAF1	Non-epigenetic	Non-epigenetic
Vemurafenib + Crenolanib		Launched | Phase 3	Combination: Vemurafenib + Crenolanib	pdgfr tyrosine kinase receptor inhibitor | raf inhibitor	BRAF | CSF1R | CYP2C19 | CYP3A4 | CYP3A5 | FLT3 | KIT | PDGFRA | PDGFRB | RAF1	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Venetoclax	49846579	Launched	Highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy	bcl inhibitor	BCL2	Non-epigenetic	Non-epigenetic
Venetoclax + Azacitidine		Launched	Combination: (Venetoclax) Highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy. And (Azacitidine) Nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.	bcl inhibitor | dna methyltransferase inhibitor	BCL2 | DNMT1 | DNMT3A	Writer | Non-epigenetic	DNMTi | Non-epigenetic
Venetoclax + Tedizolid		Launched	Combination: (Venetoclax) Highly potent, selective and orally bioavailable Bcl-2 inhibitor with a Ki of less than 0.01 nM. Venetoclax induces autophagy. And (Tedizolid) Novel oxazolidinone, acting through inhibition of bacterial protein synthesis by binding to 23S ribosomal RNA (rRNA) of the 50S subunit of the ribosome	bcl inhibitor | protein synthesis inhibitor	BCL2	Non-epigenetic | Non-epigenetic	Non-epigenetic | Non-epigenetic
Vinblastine	13342	Launched	Vinblastine sulfate is a cytotoxic alkaloid used against various cancer types. Vinblastine sulfate inhibits the formation of microtubule and suppresses nAChR with an IC50 of 8.9 μM	microtubule inhibitor | tubulin polymerization inhibitor	JUN | TUBA1A | TUBB | TUBD1 | TUBE1 | TUBG1	Non-epigenetic	Non-epigenetic
Vincristine	5978	Launched	Inhibitor of polymerization of mutubules by binding to tubulin with IC50 of 32μM in acell-free assay.	tubulin polymerization inhibitor	TUBA4A | TUBB	Non-epigenetic	Non-epigenetic
Vindesine	40839	Launched	Vindesine is a semisynthetic derivative of vinblastine. Vindesine is a potent anticancer agent. Vindesine can be used for the research of melanoma and lung cancer	tubulin polymerization inhibitor	TUBB | TUBB1	Non-epigenetic	Non-epigenetic
Vinorelbine	5311497	Launched	Vinorelbine (ditartrate) is an anti-mitotic agent which inhibits the proliferation of Hela cells with IC50 of 1.25 nM	tubulin polymerization inhibitor	TUBA1A | TUBA1B | TUBA1C | TUBA3C | TUBA3D | TUBA3E | TUBA4A | TUBB | TUBB1 | TUBB2A | TUBB2B | TUBB3 | TUBB4A | TUBB4B | TUBB6 | TUBB8	Non-epigenetic	Non-epigenetic
Viral Expression		N/A	Viral Gene Expression	N/A		Non-epigenetic	Non-epigenetic
Vismodegib	24776445	Launched	Vismodegib (GDC-0449) is an orally active hedgehog pathway inhibitor with an IC50 of 3 nM. Vismodegib also inhibits P-gp, ABCG2 with IC50 values of 3.0 μM and 1.4 μM, respectively	hedgehog pathway inhibitor | smoothened receptor antagonist	ABCB1 | ABCG2 | CYP2C19 | CYP2C8 | DHH | IHH | PTCH1 | SMO	Non-epigenetic	Non-epigenetic
Vitamin D3	5280795	Launched	Vitamin D3 (Cholecalciferol; Colecalciferol) is a naturally occuring form of vitamin D. Vitamin D3 induces cell differentiation and prevents proliferation of cancer cells.	differentiation inducer	CYP2J2 | VDR	Non-epigenetic	Non-epigenetic
Volasertib	10461508	Phase 3	Highly potent Polo-like kinase 1 (PLK1) inhibitor with an IC50 of 0.87 nM, as well as the two closely related kinases PLK2 and PLK3 with IC50s of 5 and 56 nM, respectively	plk inhibitor	PLK1	Non-epigenetic	Non-epigenetic
Voreloxin	9952884	Phase 3	Voreloxin (SNS-595; Vosaroxin; AG 7352) is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis	topoisomerase inhibitor	PRKDC | TOP2A	Non-epigenetic	Non-epigenetic
Vorinostat	5311	Launched	HDAC inhibitor with IC50 of 10 nM	hdac inhibitor	HDAC1 | HDAC10 | HDAC11 | HDAC2 | HDAC3 | HDAC5 | HDAC6 | HDAC8 | HDAC9	Eraser	HDACi
Voxtalisib	16123056	Phase 1/Phase 2 | Phase 2	Voxtalisib (XL765) is a potent PI3K inhibitor, which has a similar activity toward class I PI3K (IC50s=39, 113, 9 and 43 nM for p110α, p110β, p110γ and p110δ, respectively), also inhibits DNA-PK (IC50=150 nM) and mTOR (IC50=157 nM). Voxtalisib (XL765) inhibits mTORC1 and mTORC2 with IC50s of 160 and 910 nM, respectively	mtor inhibitor | pi3k inhibitor	MTOR | PIK3CA | PIK3CG	Non-epigenetic	Non-epigenetic
VTP50469	132212900	Preclinical	VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity.	menin-mll interaction inhibitor	MEN1	Non-epigenetic	Non-epigenetic
WIN 64338 hydrochloride	9832172	Preclinical	WIN 64338 hydrochloride is a potent, selective, nonpeptide competitive antagonist of bradykinin B2 receptor. WIN 64338 hydrochloride inhibits [3H]-Bradykinin binding to the bradykinin B2 receptor on human IMR-90 cells with a Ki of 64 nM. WIN 64338 hydrochloride also can inhibits [3H]Quinuclidinyl benzilate binding to the rat brain muscarinic receptor (Ki=350 nM)	bradykinin receptor antagonist	BDKRB2	Non-epigenetic	Non-epigenetic
Wiskostatin	2775510	Preclinical	Wiskostatin is a potent and selective inhibitor of neuronal Wiskott-Aldrich syndrome protein (N-WASP)-mediated actin polymerization. Wiskostatin causes a rapid, profound, and irreversible decrease in cellular ATP levels	actin related protein inhibitor | neural wiskott-aldrich syndrome protein inhibitor	WASL	Non-epigenetic	Non-epigenetic
Y-27632	448042	Preclinical	ROCK1 (p160ROCK) inhibitor with Ki of 140 nM, exhibits >200-fold selectivity over other kinases, including PKC, cAMP-dependent protein kinase, MLCK and PAK	rho associated kinase inhibitor	LRRK2 | PKIA | PKN2 | PRKACA | PRKCE | ROCK1 | ROCK2	Non-epigenetic	Non-epigenetic
YK-4-279	44632017	Preclinical	Inhibitor of EWS-FLI1 binding to RNA helicase A (RHA)	apoptosis inhibitor	EWSR1 | FLI1	Non-epigenetic	Non-epigenetic
YKL-5-124	121443990	Preclinical	YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status.	cdk inhibitor	CDK2 | CDK7 | CDK9	Non-epigenetic	Non-epigenetic
YM-155	11178236	Phase 2	Inhibits Survivin promoter activity with IC50 of 0.54 nM; does not significantly inhibit SV40 promoter activity, but is observed to slightly inhibit the interaction of Survivin with XIAP. Phase 1/2.	survivin inhibitor	BIRC5	Non-epigenetic	Non-epigenetic
Z-L-Phe-CMK		Preclinical	Z-L-Phe-CMK is an inhibitor of severe acute respiratory syndrome coronavirus (SARS-CoV) main protease (Mpro), also known as 3C-like protease (3CLpro; Ki = 306 nM).1 It is selective for SARS-CoV Mpro over calpain, trypsin, and thrombin (Kis = 10, >100, and >100 µM, respectively). Z-L-Phe-CMK (20 µM) also inhibits the protein-protein interaction between p53 and MDM2 in U2OS osteosarcoma cells.2 It has been used as a building block in the synthesis of HIV protease inhibitors	protease inhibitor	3CL	Non-epigenetic	Non-epigenetic
Zibotentan	9910224	Phase 3	Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research	endothelin receptor antagonist	EDNRA	Non-epigenetic	Non-epigenetic
ZK-93423	121926	Phase 3	ZK 93423 is a potent benzodiazepine GABAA receptor agonist with a certain cooling effect on rodents	benzodiazepine receptor agonist	GABRA1 | GABRA2 | GABRA3 | GABRA5 | GABRB2 | GABRG2	Non-epigenetic	Non-epigenetic