m6A-centered Crosstalk Information
Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
| Crosstalk ID |
M6ACROT03634
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[1], [2] | |||
Histone modification
H3K27me3
EZH2
miR-338-5p
Indirect
Enhancement
m6A modification
BCL2
BCL2
METTL3
Methylation
: m6A sites
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| m6A Modification: | |||||
|---|---|---|---|---|---|
| m6A Regulator | Methyltransferase-like 3 (METTL3) | WRITER | |||
| m6A Target | Apoptosis regulator Bcl-2 (BCL2) | ||||
| Epigenetic Regulation that have Cross-talk with This m6A Modification: | |||||
| Epigenetic Regulation Type | Histone modification (HistMod) | ||||
| Epigenetic Regulator | Histone-lysine N-methyltransferase EZH2 (EZH2) | WRITER | View Details | ||
| Regulated Target | Histone H3 lysine 27 trimethylation (H3K27me3) | View Details | |||
| Downstream Gene | miR-338-5p | View Details | |||
| Crosstalk Relationship | Histone modification → m6A | Enhancement | |||
| Crosstalk Mechanism | histone modification indirectly regulates m6A modification through downstream signaling pathways | ||||
| Crosstalk Summary | Collectively, EZH2 downregulated hsa-miR-338-5p through Histone H3 lysine 27 trimethylation (H3K27me3), which in turn impaired miR-338-5p-dependent METTL3 inhibition and enhanced CDCP1 translation, therefore contributing to the development of GC. Down-regulation of METTL3 inhibits the proliferation and mobility of human gastric cancer cells and leads to inactivation of the AKT signaling pathway, suggesting that METTL3 is a potential target for the treatment of human gastric cancer. METTL3 knockdown decreased Apoptosis regulator Bcl-2 (BCL2) and increased Bax and active Caspase-3 in gastric cancer cells, which suggested the apoptotic pathway was activated. METTL3 led to inactivation of the AKT signaling pathway in human gastric cancer cells, including decreased phosphorylation levels of AKT and expression of down-stream effectors p70S6K and Cyclin D1. | ||||
| Responsed Disease | Gastric cancer | ICD-11: 2B72 | |||
| Pathway Response | Apoptosis | hsa04210 | |||
| PI3K-Akt signaling pathway | hsa04151 | ||||
| Cell Process | Cell proliferation | ||||
| Cell migration | |||||
| Cell invasion | |||||
In-vitro Model |
AGS | Gastric adenocarcinoma | Homo sapiens | CVCL_0139 | |
| MKN45 | Gastric adenocarcinoma | Homo sapiens | CVCL_0434 | ||
Full List of Potential Compound(s) Related to This m6A-centered Crosstalk
| Apoptosis regulator Bcl-2 (BCL2) | 49 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| GDC-0199 | Approved | [3] | ||
| MOA | Modulator | |||
| Activity | Ki < 0.01 nM | |||
| External Link | ||||
| MCI-186 | Approved | [4] | ||
| Synonyms |
Edarabone; Edaravone; Methylphenylpyrazolone; Monopyrazolone; Norantipyrine; Norphenazone; Phenylmethylpyrazolone; Radicut; Developer Z; Edaravone [INN]; Phenyl methyl pyrazolone; CDS1_000986; CI Developer 1; IN1263; M0687; MCI 186; Edaravone(jan); Radicut (TN); AE-641/00371017; C.I. Developer 1; Edaravone (JAN/INN); (MCI-186); 1-Fenyl-3-methyl-2-pyrazolin-5-on; 1-Fenyl-3-methyl-2-pyrazolin-5-on [Czech]; 1-Phenyl-3-methyl-5-oxo-2-pyrazoline; 1-Phenyl-3-methyl-5-pyrazolone; 1-Phenyl-3-methylpyrazolone; 1-Phenyl-3-methylpyrazolone-5; 2,4-Dihydro-5-methyl-2-phenyl-3H-pyrazol-3-one; 3-METHYL-1-PHENYL-2-PYRAZOLIN-5-ONE; 3-Methyl-1-phenyl-2-pyrazoline-5-one; 3-Methyl-1-phenyl-5-pyrazolone; 3-Methyl-1-phenylpyrazol-5-one; 5-Methyl-2-phenyl-2,4-dihydro-3H-pyrazol-3-one; 5-methyl-2-phenyl-4H-pyrazol-3-one
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| MOA | Regulator (upregulator) | |||
| External Link | ||||
| Taxol | Approved | [5] | ||
| Synonyms |
C47H51NO14; weekly paclitaxel; Micellar Paclitaxel; Paclitaxel [USAN:INN:BAN]; SCHEMBL15000506; Benzenepropanoic acid, beta-(benzoylamino)-alpha-hydroxy-, 6,12b-bis(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca(3,4)benz(1,2-b)oxet-9-yl ester, (2aR-(2aalpha,4beta,4abeta,6beta,9alpha(alphaR*,betaS*),11alpha,12alpha,12aalpha,12balpha))-
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| MOA | Modulator | |||
| External Link | ||||
| Oblimersen | Phase 3 | [6] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| RG7601 | Phase 3 | [3] | ||
| MOA | Modulator | |||
| External Link | ||||
| Taxol/Paraplatin/Herceptin | Phase 3 | [7] | ||
| Synonyms |
Paclitaxel/carboplatin/trastuzumab
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| MOA | Modulator | |||
| External Link | ||||
| ABT-263 | Phase 3 | [8] | ||
| Synonyms |
Navitoclax; ABT 263; S1001_Selleck; ABT263, Navitoclax; 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-en-1-yl]methyl}piperazin-1-yl)-N-({4-({(1R)-3-morpholin-4-yl-1-[(phenylsulfanyl)methyl]propyl}amino)-3-[(trifluoromethyl)sulfonyl]phenyl}sulfonyl)benzamide
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| MOA | Inhibitor | |||
| Activity | Ki < 0.01 nM | |||
| External Link | ||||
| Thymoquinone | Phase 2/3 | [9] | ||
| Synonyms |
490-91-5; Thymoquinon; p-Cymene-2,5-dione; 2-Isopropyl-5-methyl-1,4-benzoquinone; 2,5-CYCLOHEXADIENE-1,4-DIONE, 2-METHYL-5-(1-METHYLETHYL)-; 2-Isopropyl-5-methyl-p-benzoquinone; 2-Isopropyl-5-methylbenzoquinone; Polythymoquinone; 5-Isopropyl-2-methyl-1,4-benzoquinone; 2-Isopropyl-5-methylbenzo-1,4-quinone; p-Mentha-3,6-diene-2,5-dione; NSC 2228; 2-Isopropyl-5-methylcyclohexa-2,5-diene-1,4-dione; 2-Methyl-5-isopropyl-p-benzoquinone; 2-methyl-5-propan-2-ylcyclohexa-2,5-diene-1,4-dione; NSC2228; 2-methyl-5-(propan-2-yl)cyclohexa-2,5-diene-1,4-dione; UNII-O60IE26NUF; 2-Methyl-5-isopropyl-1,4-benzoquinone; O60IE26NUF; 2,5-Cyclohexadiene-1,4-dione, 5-isopropyl-2-methyl-; NSC-2228; 5-Isopropyl-2-methyl-p-benzoquinone; MFCD00001602; 2-Methyl-5-(1-methylethyl)-2,5-cyclohexadiene-1,4-dione; p-Mentha-3,6-diene-2,5-dione (8CI); 5-Isopropyl-2-methyl-2,5-Cyclohexadiene-1,4-dione; CCRIS 7152; EINECS 207-721-1; 2-methyl-5-(methylethyl)cyclohexa-2,5-diene-1,4-dione; BRN 1939047; thymolquinone; Thymoil; AI3-17758; 4hco; p-Mentha-3,5-dione; Spectrum_001237; SpecPlus_000457; Thymoquinone, >=98%; Spectrum2_000700; Spectrum3_001345; Spectrum4_001895; Spectrum5_000550; BSPBio_003129; KBioGR_002455; KBioSS_001717; DivK1c_006553; SCHEMBL542535; SPBio_000859; CHEMBL1672002; DTXSID9060079; KBio1_001497; KBio2_001717; KBio2_004285; KBio2_006853; KBio3_002349; Thymoquinone, analytical standard; CHEBI:113532; 2-Methyl-5-iso-propylbenzoquinone; BDBM166686; ZINC164367; BCP16946; HY-D0803; WLN: L6V DVJ B1 EY1&1; 2,4-dione, 5-isopropyl-2-methyl-; ANW-41600; CCG-40027; s4761; SBB008296; AKOS003368628; MCULE-9899033250; NCGC00178250-01; NCGC00178250-05; 73940-92-8; AK101679; AS-11327; 2-Isopropyl-5-methylbenzo-1,4-quinone #; 2,4-dione, 2-methyl-5-(1-methylethyl)-; CS-0012226; FT-0612708; ST45023960; K-9199; SR-05000002192; Q7799650; SR-05000002192-2; W-202869; BRD-K97566842-001-03-5; 2-methyl-5-(propan-2-yl)cyclohexa-2,5-diene-1,4-dione (F8); 2-Methyl-5-(1-methylethyl)-2,5-cyclohexadiene-1,4-dione, 9CI
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| MOA | Inhibitor | |||
| External Link | ||||
| Gossypol | Phase 2 | [10] | ||
| Synonyms |
303-45-7; (-)-Gossypol; 90141-22-3; (+)-Gossypol; Pogosin; Tash 1; racemic-Gossypol; (R)-(-)-Gossypol; (R)-Gossypol; (+-)-Gossypol; (+/-)-Gossypol; CCRIS 2689; NSC56817; NSC 56817; NSC 624336; BRN 1917878; CHEMBL51483; AI3-22957; 20300-26-9; 1,1',6,6',7,7'-Hexahydroxy-5,5'-diisopropyl-3,3'-dimethyl-[2,2'-binaphthalene]-8,8'-dicarbaldehyde; 2,2'-bi[8-Formyl-1,6,7-trihydroxy-5-isopropyl-3-methylnaphthalene]; 2,2'-Bis(1,6,7-trihydroxy-3-methyl-5-isopropyl-8-aldehydonaphthalene); NSC624336; Gossypol acetate
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| MOA | Regulator | |||
| Activity | Ki = 170 nM | |||
| External Link | ||||
| PI-88/Taxotere | Phase 2 | [11] | ||
| Synonyms |
PI-88/docetaxel
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| MOA | Modulator | |||
| External Link | ||||
| Obatoclax | Phase 2 | [12] | ||
| Synonyms |
CHEMBL408194; UNII-QN4128B52A; QN4128B52A; SCHEMBL631676; SCHEMBL16340850; BDBM50376902; ZINC136873052; DB12191; NCGC00387855-01; BRD-K15600710-066-01-7
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| MOA | Inhibitor | |||
| Activity | EC50 = 300 nM | |||
| External Link | ||||
| APG-2575 | Phase 1/2 | [13] | ||
| Synonyms |
Bcl-2/Bcl-xl inhibitor 1; 2180923-05-9; OSL3FEZ1IF; UNII-OSL3FEZ1IF; SCHEMBL20580489; US10221174, Compound 6; BDBM361577; HY-129179; CS-0103865; (S)-N-((4-(((1,4-dioxan-2-yl)methyl)amino)-3- nitrophenyl)sulfonyl)-2-((1H-pyrrolo[2,3-b]pyridin- 5-yl)oxy)-4-(4-((6-(4-chlorophenyl)spiro[3.5]non-6- en-7-yl)methyl)piperazin-1-yl)benzamide; Benzamide, 4-(4-((6-(4-chlorophenyl)spiro(3.5)non-6-en-7-yl)methyl)-1-piperazinyl)-N-((4-(((2S)-1,4-dioxan-2-ylmethyl)amino)-3-nitrophenyl)sulfonyl)-2-(1H-pyrrolo(2,3-b)pyridin-5-yloxy)-
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| MOA | Inhibitor | |||
| External Link | ||||
| APG-1252 | Phase 1/2 | [14] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| AZD0466 | Phase 1/2 | [15] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| BCL201 | Phase 1 | [16] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| Pc4 | Phase 1 | [17] | ||
| Synonyms |
Pc4 (topical formulation, cancer/psoriasis/dermatological disease) Fluence/CWRU/UHCMC
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| MOA | Agonist | |||
| External Link | ||||
| BGB-11417 | Phase 1 | [18] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| LP-108 | Phase 1 | [19] | ||
| External Link | ||||
| LOXO-338 | Phase 1 | [20] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| VOB560 | Phase 1 | [21] | ||
| Synonyms |
S 65487
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| MOA | Inhibitor | |||
| External Link | ||||
| AI-850 | Phase 1 | [22] | ||
| MOA | Modulator | |||
| External Link | ||||
| Irofulven/Taxotere | Phase 1 | [23] | ||
| Synonyms |
MGI 114/docetaxel
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| MOA | Modulator | |||
| External Link | ||||
| Indole-based analog 2 | Patented | [24] | ||
| Synonyms |
PMID27744724-Compound-16
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| MOA | Inhibitor | |||
| Activity | Ki = 7100 nM | |||
| External Link | ||||
| PMID27744724-Compound-10 | Patented | [24] | ||
| MOA | Inhibitor | |||
| Activity | Ki = 5800 nM | |||
| External Link | ||||
| PMID27744724-Compound-21 | Patented | [24] | ||
| MOA | Inhibitor | |||
| Activity | Ki = 2000 nM | |||
| External Link | ||||
| Indole-based analog 3 | Patented | [24] | ||
| Synonyms |
PMID27744724-Compound-17
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| MOA | Inhibitor | |||
| Activity | Ki = 1900 nM | |||
| External Link | ||||
| PMID27744724-Compound-18 | Patented | [24] | ||
| MOA | Inhibitor | |||
| Activity | Ki = 33000 nM | |||
| External Link | ||||
| ABT-737 | Terminated | [25] | ||
| Synonyms |
852808-04-9; ABT 737; ABT737; UNII-Z5NFR173NV; Z5NFR173NV; 4-[4-[(4'-Chloro[1,1'-biphenyl]-2-yl)methyl]-1-piperazinyl]-N-[[4-[[(1R)-3-(dimethylamino)-1-[(phenylthio)methyl]propyl]amino]-3-nitrophenyl]sulfonyl]benzamide; CHEMBL376408; C42H45ClN6O5S2; 4-{4-[(4'-Chlorobiphenyl-2-Yl)methyl]piperazin-1-Yl}-N-{[4-({(1r)-3-(Dimethylamino)-1-[(Phenylthio)methyl]propyl}amino)-3-Nitrophenyl]sulfonyl}benzamide
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| MOA | Inhibitor | |||
| Activity | Ki < 0.6 nM | |||
| External Link | ||||
| WL-276 | Investigative | [26] | ||
| MOA | Modulator | |||
| External Link | ||||
| N-phenyl-2,3,4-trihydroxy-5-benzyl-benzamide | Investigative | [27] | ||
| Synonyms |
CHEMBL214965; SCHEMBL15313847
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| MOA | Inhibitor | |||
| Activity | IC50 = 5000 nM | |||
| External Link | ||||
| 5,10-Dioxy-2-phenyl-benzo[g]pteridin-4-ylamine | Investigative | [28] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1600 nM | |||
| External Link | ||||
| modified HA14-1 compounds (cancer) | Investigative | [29] | ||
| Synonyms |
Bcl-2 inhibitor (cancer), GL Pharmaceuticals; HA14-1, GL Pharmaceuticals
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| MOA | Modulator | |||
| External Link | ||||
| Apogossypol | Investigative | [30] | ||
| Synonyms |
BI-79D10; BI-97C1; CNDO-103; CNDO-133
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| MOA | Inhibitor | |||
| Activity | Ki = 640 nM | |||
| External Link | ||||
| 2,3,4-trihydroxy-5-isopropyl-N-phenyl-benzamide | Investigative | [27] | ||
| Synonyms |
CHEMBL214839; BDBM50196033
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| MOA | Inhibitor | |||
| Activity | IC50 = 7000 nM | |||
| External Link | ||||
| 4,5-dibenzylbenzene-1,2-diol | Investigative | [31] | ||
| Synonyms |
4,5-Dibenzyl-1,2-benzenediol; NSC664154; AC1L8EAW; CHEMBL481409; AC1Q79U2; SCHEMBL18604567; CTK7J8443; BDBM34138; 4,5-dibenzylbenzene-1,2-diol, 9; NSC-664154
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| MOA | Inhibitor | |||
| Activity | IC50 = 4700 nM | |||
| External Link | ||||
| TW-37 | Investigative | [27] | ||
| Synonyms |
877877-35-5; N-[4-(2-tert-Butylphenylsulfonyl)phenyl]-2,3,4-trihydroxy-5-(2-isopropylbenzyl)benzamide; tw 37; CHEMBL217354; N-(4-((2-(tert-butyl)phenyl)sulfonyl)phenyl)-2,3,4-trihydroxy-5-(2-isopropylbenzyl)benzamide; N-(4-(2-tert-butylphenylsulfonyl)phenyl)-2,3,4-trihydroxy-5-(2-isopropylbenzyl)benzamide; N-[4-[(2-tert-Butylphenyl)sulfonyl]phenyl]-2,3,4-trihydroxy-5-[(2-isopropylphenyl)methyl]benzamide; N-(4-((2-Tert-Butylphenyl)sulfonyl)phenyl)-2,3,4-trihydroxy-5-((2-isopropylphenyl)methyl)benzamide
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| MOA | Inhibitor | |||
| Activity | IC50 = 200 nM | |||
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| QEDIIRNIARHLAQVGDSMDR | Investigative | [27] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PNT-2258 | Phase 2 | [32] | ||
| External Link | ||||
| Beclanorsen | Phase 1/2 | [32] | ||
| Synonyms |
SPC-2004; SPC-2993; SPC-2996; Anti-Bcl-2 (LNA antisense therapy), Santaris
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| BP1002 | Phase 1 | [32] | ||
| External Link | ||||
| G3139 + Thalidomide | Investigative | [32] | ||
| External Link | ||||
| G3139 + Irinotecan | Investigative | [32] | ||
| External Link | ||||
| G3139 + G-CSF | Investigative | [32] | ||
| External Link | ||||
| G3139 + Fludarabine | Investigative | [32] | ||
| External Link | ||||
| BP-100-1.02 | Investigative | [32] | ||
| Synonyms |
Liposomal Bcl-2 (lymphoma/solid tumor), Bio-Path
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| External Link | ||||
| G3139 + Paclitaxel | Investigative | [32] | ||
| External Link | ||||
| G3139 + Dexamethasone | Investigative | [32] | ||
| External Link | ||||
| G3139 + Dacarbazine | Investigative | [32] | ||
| External Link | ||||
| G3139 + cytarabine (ARA-C) | Investigative | [32] | ||
| External Link | ||||
| Histone-lysine N-methyltransferase EZH2 (EZH2) | 74 Compound(s) Regulating the Target | Click to Show/Hide the Full List | ||
| Tazemetostat | Approved | [33] | ||
| Synonyms |
EPZ-6438; 1403254-99-8; EPZ6438; UNII-Q40W93WPE1; N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide; Q40W93WPE1; EPZ 6438; E7438; (1,1'-Biphenyl)-3-carboxamide, N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(4-morpholinylmethyl)-
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| MOA | Inhibitor | |||
| Activity | Ki = 2.5 nM | |||
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| DS-3201b | Phase 2 | [34] | ||
| Synonyms |
Valemetostat; 1809336-39-7; UNII-60RD0234VE; 60RD0234VE; 1809336-39-7 (free base); DS-3201; (2R)-7-chloro-2-[trans-4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide; Valemetostat 2HCl; Valemetostat [INN]; Valemetostat (DS-3201); CHEMBL4597193; EZH1/2 inhibitor DS-3201; SCHEMBL18393626; SCHEMBL18393627; SCHEMBL18639210; EX-A3423; DS3201; NSC813381; s8926; NSC-813381; HY-109108; CS-0039740; D11551
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| MOA | Inhibitor | |||
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| CPI-1205 | Phase 1/2 | [16] | ||
| Synonyms |
HPODOLXTMDHLLC-QGZVFWFLSA-N; 1621862-70-1; UNII-455J2479FY; CPI1205; CPI 1205; 455J2479FY; (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide; GTPL9115; SCHEMBL17329268; MolPort-044-560-382; KS-000006BA; EX-A1068; s8353; AKOS030628484; ZINC220982768; CS-7648; compound 13 [PMID: 27739677]; HY-100021; J3.556.402K; N-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-2-methyl-1-[(1R)-1-[1-(2,2,2-trifluoroethyl)piperidin-4-
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| MOA | Inhibitor | |||
| External Link | ||||
| SHR2554 | Phase 1/2 | [35] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| CPI-0209 | Phase 1/2 | [36] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| GSK2816126 | Phase 1 | [37] | ||
| Synonyms |
GSK 126; GSK-126
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| MOA | Modulator | |||
| Activity | Ki = 0.5 nM | |||
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| PF-06821497 | Phase 1 | [38] | ||
| Synonyms |
UNII-S4L4MM20B6; S4L4MM20B6; CHEMBL4080228; PF06821497; 1844849-10-0; 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1(2H)-one; SCHEMBL17330426; GTPL10516; BDBM50246967; NSC800019; DB14799; HY-101571A; NSC-800019; compound 23a [PMID: 29211475]; CS-0092626; Q29209799; 1(2H)-Isoquinolinone, 5,8-dichloro-2-((1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl)-3,4-dihydro-7-((R)-methoxy-3-oxetanylmethyl)-; 5,8-dichloro-2-[(4-methoxy-6-methyl-2-oxo-1H-pyridin-3-yl)methyl]-7-[(R)-methoxy(oxetan-3-yl)methyl]-3,4-dihydroisoquinolin-1-one; CJD
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| MOA | Inhibitor | |||
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| DS-3201 | Phase 1 | [16] | ||
| Synonyms |
QTGYNKYZRZATJB-UHFFFAOYSA-N; 701899-63-0; 2-(2-(2-Methyl-1H-imidazol-5-yl)ethyl)isoindoline-1,3-dione; 2-(2-(2-Methyl-1H-imidazol-5-yl)-ethyl)isoindoline-1,3-dione; SCHEMBL7743461; MolPort-035-945-474; MolPort-035-690-353; ZINC98086069; AKOS024459002; AKOS024262663; MCULE-2708350770; FCH4077443; AK158834; AX8292467; ST2403812; 2-[2-(2-methyl-1H-imidazol-5-yl)ethyl]-2,3-dihydro-1H-isoindole-1,3-dione
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| MOA | Inhibitor | |||
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| HH2853 | Phase 1 | [39] | ||
| MOA | Inhibitor | |||
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| PMID28394193-Compound-33 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 100 nM | |||
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| PMID28394193-Compound-Figure3bI | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-35 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 10 nM | |||
| External Link | ||||
| PMID28394193-Compound-54 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-24 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-27 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-25 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-50 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM | |||
| External Link | ||||
| PMID28394193-Compound-47 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 2 nM; Ki < 1 nM | |||
| External Link | ||||
| PMID28394193-Compound-21 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-41 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-53 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 80 nM | |||
| External Link | ||||
| PMID28394193-Compound-Figure5aVIII | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-38 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-51 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM | |||
| External Link | ||||
| PMID28394193-Compound-31 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 20 nM | |||
| External Link | ||||
| PMID28394193-Compound-42 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-15 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-52 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM | |||
| External Link | ||||
| PMID28394193-Compound-32 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 500 nM | |||
| External Link | ||||
| PMID28394193-Compound-23 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-29 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 100 nM | |||
| External Link | ||||
| PMID28394193-Compound-30 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 16 nM | |||
| External Link | ||||
| PMID28394193-Compound-39 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-49 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM | |||
| External Link | ||||
| PMID28394193-Compound-43 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-40 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-Figure3bIII | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-36 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 316 nM | |||
| External Link | ||||
| PMID28394193-Compound-28 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 32 nM | |||
| External Link | ||||
| PMID28394193-Compound-22 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-18 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-16 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-44 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-20 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-19 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-37 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-Figure3bII | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-26 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 1000 nM | |||
| External Link | ||||
| PMID28394193-Compound-17 | Patented | [40] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-34 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 100 nM | |||
| External Link | ||||
| PMID28394193-Compound-56 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 0.93 nM | |||
| External Link | ||||
| PMID28394193-Compound-46 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 5 nM | |||
| External Link | ||||
| PMID28394193-Compound-57 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 6.45 nM | |||
| External Link | ||||
| PMID28394193-Compound-14 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 21900 nM | |||
| External Link | ||||
| PMID28394193-Compound-12 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 10 nM | |||
| External Link | ||||
| PMID26882240-Compound-1 | Patented | [41] | ||
| MOA | Inhibitor | |||
| External Link | ||||
| PMID28394193-Compound-55 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 8.13 nM | |||
| External Link | ||||
| PMID28394193-Compound-45 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 168000 nM | |||
| External Link | ||||
| PMID28394193-Compound-13 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1470 nM | |||
| External Link | ||||
| EPZ005687 | Investigative | [42] | ||
| Synonyms |
EPZ-005687; EPZ 005687
Click to Show/Hide
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| MOA | Inhibitor | |||
| External Link | ||||
| EI1 | Investigative | [43] | ||
| Synonyms |
KB-145943
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| MOA | Inhibitor | |||
| External Link | ||||
| UNC1999 | Investigative | [44] | ||
| Synonyms |
UNC 1999; UNC-1999
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| MOA | Inhibitor | |||
| External Link | ||||
| MS1943 | Investigative | [35] | ||
| Synonyms |
2225938-17-8; SCHEMBL21271666; EX-A3962; s8918; HY-133129; CS-0112146; 6-(6-(4-(2-(2-((3r,5r,7r)-adamantan-1-yl)acetamido)ethyl)piperazin-1-yl)pyridin-3-yl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-1H-indazole-4-carboxamide; 6-(6-(4-(2-(2-(Adamantan-1-yl)acetamido)ethyl)piperazin-1-yl)pyridin-3-yl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-isopropyl-1H-indazole-4-carboxamide
Click to Show/Hide
|
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| MOA | Degrader | |||
| External Link | ||||
| GSK343 | Investigative | [45] | ||
| Synonyms |
compound 6 [PMID 24900432]; GSK 343
Click to Show/Hide
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| MOA | Inhibitor | |||
| Activity | IC50 = 174 nM | |||
| External Link | ||||
| PMID28394193-Compound-11 | Patented | [32] | ||
| External Link | ||||
| PMID28394193-Compound-10 | Patented | [32] | ||
| External Link | ||||
| PMID28394193-Compound-14 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 21900 nM | |||
| External Link | ||||
| PMID28394193-Compound-12 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 < 10 nM | |||
| External Link | ||||
| PMID28394193-Compound-13 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 1470 nM | |||
| External Link | ||||
| PMID28394193-Compound-56 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 0.93 nM | |||
| External Link | ||||
| PMID28394193-Compound-46 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 5 nM | |||
| External Link | ||||
| PMID28394193-Compound-57 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 6.45 nM | |||
| External Link | ||||
| PMID28394193-Compound-55 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 8.13 nM | |||
| External Link | ||||
| PMID28394193-Compound-45 | Patented | [40] | ||
| MOA | Inhibitor | |||
| Activity | IC50 = 168000 nM | |||
| External Link | ||||
| 2B72: Gastric cancer | 81 Compound(s) Regulating the Disease | Click to Show/Hide the Full List | ||
| Leniolisib | Approved | [46] | ||
| Synonyms |
1354690-24-6; Leniolisib free base; UNII-L22772Z9CP; (S)-1-(3-((6-(6-methoxy-5-(trifluoromethyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)propan-1-one; L22772Z9CP; 1354690-24-6 (free base); leniolisib(CDZ 173); CDZ173; CDZ-173; 1-[(3S)-3-[[6-[6-methoxy-5-(trifluoromethyl)pyridin-3-yl]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-4-yl]amino]pyrrolidin-1-yl]propan-1-one; Leniolisib [INN]; Leniolisib (CDZ173); Leniolisib (USAN/INN); CDZ173-NX; SCHEMBL323054; GTPL9424; CHEMBL3643413; BDBM118299; EX-A2854; MFCD30470232; s8752; ZB1510; CS-7524; DC22326; SB18839; Example 67 [WO2012004299]; 1-{(S)-3-[6-(6-methoxy-5-trifluoromethyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-y; 1-{(S)-3-[6-(6-methoxy-5-trifluoromethyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-ylamino]-pyrrolidin-1-yl}-propan-1-one; AS-56217; HY-17635; A16796; D11158; US8653092, 67; Q27282602; 1-Propanone, 1-((3S)-3-((5,6,7,8-tetrahydro-6-(6-methoxy-5-(trifluoromethyl)-3-pyridinyl)pyrido(4,3-d)pyrimidin-4-yl)amino)-1-pyrrolidinyl)-; 9NQ
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| External Link | ||||
| Atezolizumab | Approved | [16] | ||
| External Link | ||||
| Bavencio | Approved | [16] | ||
| External Link | ||||
| Tebentafusp | Approved | [47] | ||
| External Link | ||||
| Merimepodib | Approved | [48] | ||
| Synonyms |
Merimebodib; Merimepodib [USAN:INN]; Tyverb/Tykerb; MMPD; 198821-22-6; 2ZL2BA06FU; C23H24N4O6; CHEMBL304087; MERIMEPODIB, VI-21497, VX-497; UNII-2ZL2BA06FU; VI-21497; VX-497; VX497; Vx 497; carbamic acid
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| External Link | ||||
| Taxol | Approved | [49] | ||
| Synonyms |
C47H51NO14; weekly paclitaxel; Micellar Paclitaxel; Paclitaxel [USAN:INN:BAN]; SCHEMBL15000506; Benzenepropanoic acid, beta-(benzoylamino)-alpha-hydroxy-, 6,12b-bis(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca(3,4)benz(1,2-b)oxet-9-yl ester, (2aR-(2aalpha,4beta,4abeta,6beta,9alpha(alphaR*,betaS*),11alpha,12alpha,12aalpha,12balpha))-
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| External Link | ||||
| Ramucirumab | Approved | [50] | ||
| Synonyms |
LY3009806
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| External Link | ||||
| Tucatinib | Approved | [51] | ||
| Synonyms |
Irbinitinib; 937263-43-9; ONT-380; UNII-234248D0HH; 234248D0HH; N6-(4,4-Dimethyl-4,5-dihydrooxazol-2-yl)-N4-(3-methyl-4-((1,2,4)triazolo(1,5-a)pyridin-7-yloxy)phenyl)quinazoline-4,6-diamine; 4,6-Quinazolinediamine, N6-(4,5-dihydro-4,4-dimethyl-2-oxazolyl)-N4-(3-methyl-4-((1,2,4)triazolo(1,5-a)pyridin-7-yloxy)phenyl)-; ONT 380; 4,6-QuinazolinediaMine, N6-(4,5-dihydro-4,4-diMethyl-2-oxazolyl)-N4-[3-Methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)phenyl]-; Tucatinib [USAN:INN]; 6-DIAMINE
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| External Link | ||||
| Antacids | Approved | [52] | ||
| External Link | ||||
| Trastuzumab | Approved | [16] | ||
| Synonyms |
Herceptin; Herceptin (TN); Trastuzumab (INN); Trastuzumab (genetical recombination); Trastuzumab (genetical recombination) (JAN); Trastuzumab (ERBB2 mAb inhibitor)
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| External Link | ||||
| Carbamazepine | Phase 3 | [53] | ||
| Synonyms |
Carbamazepine (iv, epilepsy); Carbamazepine (iv, epilepsy), Lundbeck; Carbamazepine (iv, epilepsy), Ovation Pharmaceuticals
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| External Link | ||||
| Margetuximab | Approved | [16] | ||
| External Link | ||||
| Nivolumab | Approved | [16] | ||
| External Link | ||||
| GRANITE | Phase 3 | [54] | ||
| Synonyms |
Penoxsulam; 219714-96-2; 2-(2,2-difluoroethoxy)-N-(5,8-dimethoxy-[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)-6-(trifluoromethyl)benzenesulfonamide; UNII-784ELC1SCZ; 784ELC1SCZ; CHEBI:81776; 2-(2,2-difluoroethoxy)-n-(5,8-dimethoxy[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)-6-(trifluoromethyl)benzenesulfonamide; Penoxsulam [ISO]; PXD; DSSTox_CID_14803; DSSTox_RID_79204; DSSTox_GSID_34803; SCHEMBL116968; CHEMBL1895913; DTXSID0034803; HSDB 7887; AMY12535; BCP18718; EBD18529; Tox21_301010; MFCD07363876; ZINC13827750; AKOS025401685; NCGC00163715-01; NCGC00163715-02; NCGC00163715-03; NCGC00254912-01; AC-24494; Penoxsulam 100 microg/mL in Acetonitrile; CAS-219714-96-2; FT-0696708; Penoxsulam, PESTANAL(R), analytical standard; C18481; Q22808507; 2-(2,2-Difluoroethoxy)-6-trifluoromethyl-N-(5, 8-dimethoxy[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)benzenesulfonamide; 2-(2,2-Difluoroethoxy)-N-(5,8-dimethoxy[1,2,4]-triazolo[1,5-c]pyrimidin-2-yl)-6-(trifluoromethyl)benzenesulfonamide; 2-(2,2-difluoroethoxy)-N-{5,8-dimethoxy-[1,2,4]triazolo[1,5-c]pyrimidin-2-yl}-6-(trifluoromethyl)benzene-1-sulfonamide; 2-(2,2-difluoroethyl)-N-(5,8-dimethoxy[1,2,4]triazolo[1,5-c]pyrimidin-2-yl)-6-(trifluoromethyl)benzenesulfonamide; Benzenesulfonamide, 2-(2,2-difluoroethoxy)-N-(5,8-dimethoxy(1,2,4)triazolo(1,5-c)pyrimidin-2-yl)-6-(trifluoromethyl)-
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| External Link | ||||
| Zolbetuximab | Phase 3 | [55] | ||
| Synonyms |
IMAB362
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| External Link | ||||
| Tusamitamab ravtansine | Phase 3 | [56] | ||
| Synonyms |
SAR408701
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| External Link | ||||
| Andecaliximab | Phase 3 | [57] | ||
| External Link | ||||
| ABP 980 | Phase 3 | [58] | ||
| External Link | ||||
| GS-5745 | Phase 3 | [49] | ||
| External Link | ||||
| S-1 | Phase 3 | [59] | ||
| Synonyms |
Ciprofibrate-coa; Ciprofibrate-coenzyme A; Coenzyme A, ciprofibrate-; AC1L4TRG; AC1Q3T4H; 111900-25-5; s-{1-[(2r,3s,4r,5r)-5-(6-amino-9h-purin-9-yl)-4-hydroxy-3-(phosphonooxy)tetrahydrofuran-2-yl]-3,5,9-trihydroxy-8,8-dimethyl-3,5-dioxido-10,14-dioxo-2,4,6-trioxa-11,15-diaza-3; E5,5; E5-diphosphaheptadecan-17-yl} 2-[4-(2,2-dichlorocyclopropyl)phenoxy]-2-methylpropanethioate(non-preferred name); Coenzyme A, S-(2-(4-(2,2-dichlorocyclopropyl)phenoxy)-2-methylpropanoate)
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| External Link | ||||
| Lonsurf | Phase 3 | [16] | ||
| External Link | ||||
| GDC-0068 | Phase 3 | [49] | ||
| Synonyms |
RG7440
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| External Link | ||||
| Edotecarin | Phase 3 | [60] | ||
| Synonyms |
ED-749; Edotecarin < Prop INN; J-107088; PF-804950; 12-(beta-D-Glucopyranosyl)-2,10-dihydroxy-6-[2-hydroxy-1-(hydroxymethyl)ethylamino]-6,7,12,13-tetrahydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7-dione
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| External Link | ||||
| RG3638 | Phase 3 | [61] | ||
| Synonyms |
Onartuzumab
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| External Link | ||||
| G17DT | Phase 3 | [62] | ||
| Synonyms |
Gastrimmune; Insegia
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| External Link | ||||
| DE-766 | Phase 3 | [63] | ||
| External Link | ||||
| Tesetaxel | Phase 2 | [64] | ||
| Synonyms |
DJ-927; 333754-36-2; UNII-UG97LO5M8Y; UG97LO5M8Y; Tesetaxel [INN]; DJ927; DJ 927; CHEMBL2107787; SCHEMBL12060837; DB12019; Z-3104; (2AS,2BR,3S,4S,6S,8AR,10R,11AS,11BR,13AR)-2A-ACETOXY-6-(((2R,3S)-3-((TERT-BUTOXYCARBONYL)AMINO)-3-(3-FLUOROPYRIDIN-2-YL)-2-HYDROXYPROPANOYL)OXY)-10-((DIMETHYLAMINO)METHYL)-4-HYDROXY-7,11B,14,14-TETRAMETHYL-2A,2B,3,4,5,6,8A,11A,11B,12,13,13A-DODECAHYDRO-2H-4,8-METHANOOXETO[3'',2'':3',4']BENZO[1',2':3,4]CYCLODECA[1,2-D][1,3]DIOXOL-3-YL BENZOATE
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| External Link | ||||
| Nelipepimut S | Phase 3 | [65] | ||
| Synonyms |
E75
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| External Link | ||||
| BMS-986205 | Phase 3 | [16] | ||
| Synonyms |
KRTIYQIPSAGSBP-KLAILNCOSA-N; 1923833-60-6; BMS986205; UNII-0A7729F42K; 0A7729F42K; GTPL9707; SCHEMBL18826792; SCHEMBL17740982; SCHEMBL19105151; EX-A2606; AKOS032954040; HY-101560; CS-0021719; Q29213697; (R)-N-(4-chlorophenyl)-2-((1s,4S)-4-(6-fluoroquinolin-4-yl)cyclohexyl)propanamide; (2R)-N-(4-chlorophenyl)-2-[4-(6-fluoroquinolin-4-yl)cyclohexyl]propanamide; (2R)-N-(4-Chlorophenyl)-2-(4-(6-fluoro-4-quinolyl)cyclohexyl)propanamide, cis; Cyclohexaneacetamide, N-(4-chlorophenyl)-4-(6-fluoro-4-quinolinyl)-alpha-methyl-, cis-(alphaR)-
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| External Link | ||||
| Rivoceranib | Phase 3 | [16] | ||
| External Link | ||||
| Claudiximab | Phase 3 | [16] | ||
| Synonyms |
IMAB-362; Anti-GC182 mAbs (cancer), Ganymed; Anti-GC182 monoclonal antibodies (cancer), Ganymed; Anti-CLDN18-2 mAbs (cancer), Ganymed; Anti-CLDN18-2 monoclonal antibodies (cancer), Ganymed
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| External Link | ||||
| OS-440 | Phase 3 | [66] | ||
| Synonyms |
CNS modulator (spasticity), Osmotica
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| External Link | ||||
| Oraxol | Phase 3 | [16] | ||
| External Link | ||||
| ICI 118,551 | Phase 3 | [49] | ||
| Synonyms |
Ici 118551; (2R,3S)-1-[(7-methyl-2,3-dihydro-1H-inden-4-yl)oxy]-3-(propan-2-ylamino)butan-2-ol; CHEMBL198059; CHEBI:73289; ICI-118551; ICI118551; erythro-DL-1-(7-Methylindan-4-yloxy)-3-isopropylaminobutan-2-ol; (2R,3S)-3-(isopropylamino)-1-[(7-methyl-2,3-dihydro-1H-inden-4-yl)oxy]butan-2-ol; 2-Butanol, 1-((2,3-dihydro-7-methyl-1H-inden-4-yl)oxy)-3-((1-methylethyl)amino)-, (2R,3S)-rel-; 2-Butanol, 1-((2,3-dihydro-7-methyl-1H-inden-4-yl)oxy)-3-((1-methylethyl)amino)-, (R*,S*)-(+-)-; ICI-118,551; Ici 111,581; AC1NUNSO
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| External Link | ||||
| Evorpacept | Phase 2/3 | [67] | ||
| Synonyms |
ALX148
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| External Link | ||||
| BNT141 | Phase 2 | [68] | ||
| External Link | ||||
| Anti-LAG3 | Phase 2 | [58] | ||
| External Link | ||||
| GSK1292263 | Phase 2 | [69] | ||
| External Link | ||||
| MM-111 | Phase 2 | [70] | ||
| External Link | ||||
| Plevitrexed | Phase 2 | [71] | ||
| Synonyms |
ZD 9331; ZD9331; 153537-73-6; Plevitrexed [INN]; ZD-9331; NSC 696259; UNII-L9P2881C3H; CHEMBL126648; (2s)-2-[(2-fluoro-4-{[(4-hydroxy-2,7-dimethylquinazolin-6-yl)methyl](prop-2-yn-1-yl)amino}benzoyl)amino]-4-(2h-tetrazol-5-yl)butanoic acid; L9P2881C3H; Plevitrexed (INN); 172521-94-7; (2S)-2-[[4-[(2,7-dimethyl-4-oxo-1H-quinazolin-6-yl)methyl-prop-2-ynylamino]-2-fluorobenzoyl]amino]-4-(2H-tetrazol-5-yl)butanoic acid; 1H-Tetrazole-5-butanoic acid,
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| DS-8201 | Phase 1 | [58] | ||
| Synonyms |
9-Aminofluorene; 9H-Fluoren-9-amine; 525-03-1; FLUOREN-9-AMINE; Fluoren-9-ylamine; UNII-4NHO2K4K5B; CCRIS 7000; BRN 2209545; 4NHO2K4K5B; OUGMRQJTULXVDC-UHFFFAOYSA-N; fluorene-9-ylamine; 9-Amino-fluoren; 9-amino-fluorene; 9H-9-fluorenamine; 9H-fluoren-9-yl-amine; AC1L1VP5; 4-12-00-03390 (Beilstein Handbook Reference); SCHEMBL353865; AC1Q53A2; AC1Q53A1; KS-00000JGC; CTK1H0380; DTXSID90200496; MolPort-001-794-448; HMS1780P20; 9H-fluoren-9-ylamine hydrochloride; ZINC1724407; ALBB-023296; CA-733; SBB005783; AKOS000264388; MCULE-8757055914; DS-
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| XL880 | Phase 2 | [72] | ||
| Synonyms |
GSK 089; GSK 1363089; GSK1363089; XL 880; GSK1363089, GSK089, foretinib, EXEL-2880, XL880; 88Z; MET inhibitors
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| Matuzumab | Phase 2 | [73] | ||
| Synonyms |
EMD-62000; EMD-72000; Anti-EGF receptor humanized antibody (iv, cancer), Merck KGaA/ Takeda Pharmaceuticals; Anti-EGFR humanized mAb (iv, cancer), Merck KGaA/ Takeda Pharmaceuticals; Anti-epidermal growth factor receptor humanized antibody (iv, cancer), Merck KGaA/ Takeda Pharmaceuticals
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| BAY-57-9352 | Phase 2 | [49] | ||
| Synonyms |
Telatinib; Bay 57-9352
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| Bemarituzumab | Phase 2 | [74] | ||
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| PEGPH20 | Phase 2 | [16] | ||
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| Plevitrexed (R)-isomer | Phase 2 | [75] | ||
| Synonyms |
YW3548
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| APR-246 | Phase 2 | [76] | ||
| Synonyms |
Eprenetapopt
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| CRS-207 | Phase 2 | [65] | ||
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| Opdivo + Yervoy | Phase 3 | [16] | ||
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| CT-041 | Phase 1/2 | [77] | ||
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| BPX-601 | Phase 1/2 | [78] | ||
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| Anti-MUC1 CAR-T cells | Phase 1/2 | [79] | ||
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| Anti-Mesothelin CAR-T cells | Phase 1/2 | [80] | ||
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| Anti-HER2 CAR-T | Phase 1/2 | [81] | ||
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| CAR-T Cells targeting EpCAM | Phase 1/2 | [82] | ||
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| PAT-SC1 | Phase 1/2 | [83] | ||
| Synonyms |
SC-1; Adjuvant therapy (gastric cancer), University of Wurzburg; SC-1 (gastric cancer), CAT; SC-1 (gastric cancer), Debiopharm; SC-1 (gastric cancer), Patrys; SC-1 (stomach cancer), OncoMab
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| ASP2138 | Phase 1 | [84] | ||
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| SAR443216 | Phase 1 | [85] | ||
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| AMG 199 | Phase 1 | [86] | ||
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| AMG 910 | Phase 1 | [87] | ||
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| Alofanib | Phase 1 | [88] | ||
| Synonyms |
1612888-66-0; 3-(N-(4-methyl-2-nitro-5-(pyridin-3-yl)phenyl)sulfamoyl)benzoic acid; RPT-835(alofanib); UNII-LQX7RFK8MZ; RPT-835; RPT835; LQX7RFK8MZ; ES000835; Alofanib [INN]; Alofanib(RPT835); Syn007154; CHEMBL4594436; SCHEMBL18660613; AMY16650; BCP31905; EX-A2731; MFCD30533418; NSC790182; s8754; Benzoic acid, 3-(((4-methyl-2-nitro-5-(3-pyridinyl)phenyl)amino)sulfonyl)-; NSC-790182; SB19665; AC-31695; AK668992; AS-56846; HY-17601; CS-0014684; RPT 835; Q27283135; 3-{[4-methyl-2-nitro-5-(pyridin-3-yl)phenyl]sulfamoyl}benzoic acid
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| HER2-specific CAR T cell | Phase 1 | [89] | ||
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| Anti-CEA-CAR T | Phase 1 | [90] | ||
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| XR-5944 | Phase 1 | [91] | ||
| Synonyms |
MLN-944; XR-11576 analogs; XR-5000 analogs; XR-5942
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| A168 | Phase 1 | [92] | ||
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| EGFR806-specific CAR T cell | Phase 1 | [93] | ||
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| AbGn-107 | Phase 1 | [16] | ||
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| FPA144 | Phase 1 | [58] | ||
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| Minnelide 001 | Phase 1 | [49] | ||
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| CAR-T cells targeting EpCAM | Phase 1 | [94] | ||
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| Anti-CEA CAR-T cells | Phase 1 | [95] | ||
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| EPCAM-targeted CAR-T cells | Clinical trial | [96] | ||
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| PMID28460551-Compound-1 | Patented | [97] | ||
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| Conjugated 3-(indolyl)-and 3-(azaindolyl)-4-arylmaleimide compound 1 | Patented | [98] | ||
| Synonyms |
PMID28621580-Compound-WO2012084683c62
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| TOPIXANTRONE HYDROCHLORIDE | Discontinued in Phase 2 | [99] | ||
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SCHEMBL1418986; Topixantrone hydrochloride < Prop INNM; BBR-3409 (dimaleate); 5-[2-(Dimethylamino)ethylamino]-2-[2-(2-hydroxyethylamino)ethyl]indazolo[4,3-gh]isoquinolin-6(2H)-one dihydrochloride
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| MDL 101,731 | Discontinued in Phase 2 | [100] | ||
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Tezacitabine; Fmdc cpd; 130306-02-4; UNII-7607Y95N9S; Mdl 101731; (E)-2'-Deoxy-2'-(fluoromethylene) cytidine; MDL-101731; 2'-Deoxy-2'-(fluoromethylene)cytidine; 7607Y95N9S; Cytidine, 2'-deoxy-2'-(fluoromethylene)-, (2E)-; (E)-2'-Deoxy-2'-(fluoromethylene)cytidine; Tezacitabine [INN]; tezaciabine; Tezacitabine, anhydrous; AC1O5KIG; SCHEMBL18724; SCHEMBL18725; Tezacitabine, anhydrous [INN]; CHEMBL2105467; C10H12FN3O4; DTXSID10156446; GFFXZLZWLOBBLO-ASKVSEFXSA-N; ZINC3777826; KW-2331
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| BBR-3438 | Discontinued in Phase 2 | [101] | ||
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Nortopixantrone; UNII-PH2639TAB4; PH2639TAB4; Nortopixantrone [INN:BAN]; AC1MI4ZO; CHEMBL150303; SCHEMBL7804438
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| IPI-493 | Discontinued in Phase 1 | [102] | ||
| Synonyms |
[(3R,5R,6S,7R,8E,10R,11R,12Z,14E)-21-amino-6-hydroxy-5,11-dimethoxy-3,7,9,15-tetramethyl-16,20,22-trioxo-17-azabicyclo[16.3.1]docosa-1(21),8,12,14,18-pentaen-10-yl] carbamate; AC1NS08X; SCHEMBL16226496; SCHEMBL16225851
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| Kanjinti | Application submitted | [16] | ||
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| Anti-CD9 mab | Investigative | [103] | ||
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ALB-6; Anti-CD9 mAb (gastric cancer); Anti-CD9 mAb (gastric cancer), Osaka University
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References
: m6A sites