Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT03638
[1], [2]
Histone modification H3K27me3 EZH2 miR-338-5p Indirect Enhancement m6A modification RPS6KB1 RPS6KB1 METTL3 Methylation : m6A sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
m6A Target Ribosomal protein S6 kinase beta-1 (RPS6KB1/p70S6K)
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 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 Ribosomal protein S6 kinase beta-1 (RPS6KB1/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
Histone-lysine N-methyltransferase EZH2 (EZH2) 74 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Tazemetostat Approved [3]
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)-
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 2.5 nM
External Link
 Compound Name DS-3201b Phase 2 [4]
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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name CPI-1205 Phase 1/2 [5]
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
 Compound Name SHR2554 Phase 1/2 [6]
MOA Inhibitor
External Link
 Compound Name CPI-0209 Phase 1/2 [7]
MOA Inhibitor
External Link
 Compound Name GSK2816126 Phase 1 [8]
Synonyms
GSK 126; GSK-126
    Click to Show/Hide
MOA Modulator
Activity Ki = 0.5 nM
External Link
 Compound Name PF-06821497 Phase 1 [9]
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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name DS-3201 Phase 1 [5]
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
External Link
 Compound Name HH2853 Phase 1 [10]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-33 Patented [11]
MOA Inhibitor
Activity IC50 = 100 nM
External Link
 Compound Name PMID28394193-Compound-Figure3bI Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-35 Patented [11]
MOA Inhibitor
Activity IC50 = 10 nM
External Link
 Compound Name PMID28394193-Compound-54 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-24 Patented [11]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
 Compound Name PMID28394193-Compound-27 Patented [11]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
 Compound Name PMID28394193-Compound-25 Patented [11]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
 Compound Name PMID28394193-Compound-50 Patented [11]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
 Compound Name PMID28394193-Compound-47 Patented [11]
MOA Inhibitor
Activity IC50 = 2 nM; Ki < 1 nM
External Link
 Compound Name PMID28394193-Compound-21 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-41 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-53 Patented [11]
MOA Inhibitor
Activity IC50 = 80 nM
External Link
 Compound Name PMID28394193-Compound-Figure5aVIII Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-38 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-51 Patented [11]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
 Compound Name PMID28394193-Compound-31 Patented [11]
MOA Inhibitor
Activity IC50 = 20 nM
External Link
 Compound Name PMID28394193-Compound-42 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-15 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-52 Patented [11]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
 Compound Name PMID28394193-Compound-32 Patented [11]
MOA Inhibitor
Activity IC50 = 500 nM
External Link
 Compound Name PMID28394193-Compound-23 Patented [11]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
 Compound Name PMID28394193-Compound-29 Patented [11]
MOA Inhibitor
Activity IC50 = 100 nM
External Link
 Compound Name PMID28394193-Compound-30 Patented [11]
MOA Inhibitor
Activity IC50 = 16 nM
External Link
 Compound Name PMID28394193-Compound-39 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-49 Patented [11]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
 Compound Name PMID28394193-Compound-43 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-40 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-Figure3bIII Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-36 Patented [11]
MOA Inhibitor
Activity IC50 = 316 nM
External Link
 Compound Name PMID28394193-Compound-28 Patented [11]
MOA Inhibitor
Activity IC50 = 32 nM
External Link
 Compound Name PMID28394193-Compound-22 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-18 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-16 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-44 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-20 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-19 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-37 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-Figure3bII Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-26 Patented [11]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
 Compound Name PMID28394193-Compound-17 Patented [11]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-34 Patented [11]
MOA Inhibitor
Activity IC50 = 100 nM
External Link
 Compound Name PMID28394193-Compound-56 Patented [11]
MOA Inhibitor
Activity IC50 = 0.93 nM
External Link
 Compound Name PMID28394193-Compound-46 Patented [11]
MOA Inhibitor
Activity IC50 = 5 nM
External Link
 Compound Name PMID28394193-Compound-57 Patented [11]
MOA Inhibitor
Activity IC50 = 6.45 nM
External Link
 Compound Name PMID28394193-Compound-14 Patented [11]
MOA Inhibitor
Activity IC50 = 21900 nM
External Link
 Compound Name PMID28394193-Compound-12 Patented [11]
MOA Inhibitor
Activity IC50 < 10 nM
External Link
 Compound Name PMID26882240-Compound-1 Patented [12]
MOA Inhibitor
External Link
 Compound Name PMID28394193-Compound-55 Patented [11]
MOA Inhibitor
Activity IC50 = 8.13 nM
External Link
 Compound Name PMID28394193-Compound-45 Patented [11]
MOA Inhibitor
Activity IC50 = 168000 nM
External Link
 Compound Name PMID28394193-Compound-13 Patented [11]
MOA Inhibitor
Activity IC50 = 1470 nM
External Link
 Compound Name EPZ005687 Investigative [13]
Synonyms
EPZ-005687; EPZ 005687
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MOA Inhibitor
External Link
 Compound Name EI1 Investigative [14]
Synonyms
KB-145943
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MOA Inhibitor
External Link
 Compound Name UNC1999 Investigative [15]
Synonyms
UNC 1999; UNC-1999
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name MS1943 Investigative [6]
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
MOA Degrader
External Link
 Compound Name GSK343 Investigative [16]
Synonyms
compound 6 [PMID 24900432]; GSK 343
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MOA Inhibitor
Activity IC50 = 174 nM
External Link
 Compound Name PMID28394193-Compound-11 Patented [17]
External Link
 Compound Name PMID28394193-Compound-10 Patented [17]
External Link
 Compound Name PMID28394193-Compound-14 Patented [11]
MOA Inhibitor
Activity IC50 = 21900 nM
External Link
 Compound Name PMID28394193-Compound-12 Patented [11]
MOA Inhibitor
Activity IC50 < 10 nM
External Link
 Compound Name PMID28394193-Compound-13 Patented [11]
MOA Inhibitor
Activity IC50 = 1470 nM
External Link
 Compound Name PMID28394193-Compound-56 Patented [11]
MOA Inhibitor
Activity IC50 = 0.93 nM
External Link
 Compound Name PMID28394193-Compound-46 Patented [11]
MOA Inhibitor
Activity IC50 = 5 nM
External Link
 Compound Name PMID28394193-Compound-57 Patented [11]
MOA Inhibitor
Activity IC50 = 6.45 nM
External Link
 Compound Name PMID28394193-Compound-55 Patented [11]
MOA Inhibitor
Activity IC50 = 8.13 nM
External Link
 Compound Name PMID28394193-Compound-45 Patented [11]
MOA Inhibitor
Activity IC50 = 168000 nM
External Link
Ribosomal protein S6 kinase beta-1 (RPS6KB1/p70S6K) 17 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name NNI-362 Phase 1 [18]
MOA Stimulator
External Link
 Compound Name M2698 Phase 1 [5]
Synonyms
HXAUJHZZPCBFPN-QGZVFWFLSA-N; 1379545-95-5; SCHEMBL15262358; EX-A1187; AKOS030627134; M2698(MSC-2363318A)
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MOA Inhibitor
External Link
 Compound Name PF-4708671 Clinical trial [19]
Synonyms
PF4708671; PF 4708671
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MOA Inhibitor
External Link
 Compound Name PMID27410995-Compound-Figure3c Patented [20]
MOA Inhibitor
External Link
 Compound Name Pyrimido[4,5-d] pyrimidines and pyrido[4,3-d] pyrimidine derivative 1 Patented [20]
Synonyms
PMID27410995-Compound-Figure3d
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MOA Inhibitor
External Link
 Compound Name SB-415286 Investigative [21]
Synonyms
SB 415286; 264218-23-7; SB415286; 3-(3-chloro-4-hydroxyphenylamino)-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione; 3-(3-chloro-4-hydroxyphenylamino)-4-(4-nitrophenyl)-1H-pyrrole-2,5-dione; CHEMBL322970; 3-(3-chloro-4-hydroxyanilino)-4-(2-nitrophenyl)pyrrole-2,5-dione; 3-[(3-chloro-4-hydroxyphenyl)amino]-4-(2-nitrophenyl)-1H-pyrrole-2,5-dione; 1H-Pyrrol-2,5-dione, 3-((3-chloro-4-hydroxyphenyl)amino)-4-(2-nitrophenyl)-; SMR000568415; SR-01000075855
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MOA Inhibitor
External Link
 Compound Name SB-747651A Investigative [22]
Synonyms
CHEMBL188434; compound 26; SCHEMBL4719834; GTPL8130; BDBM24996; oxadiazole-containing compound, 9; MBCJUIJWPYUEBX-UHFFFAOYSA-N; ZINC13998530; NCGC00273984-05; NCGC00273984-03; SB-747651; 4-{1-ethyl-7-[(piperidin-4-ylamino)methyl]-1H-imidazo[4,5-c]pyridin-2-yl}-1,2,5-oxadiazol-3-amine; [2-(4-Amino-furazan-3-yl)-1-ethyl-1H-imidazo[4,5-c]pyridin-7-ylmethyl]-piperidin-4-yl-amine
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MOA Inhibitor
Activity IC50 = 270 nM
External Link
 Compound Name ACTB-1003 Investigative [23]
Synonyms
Multi-mode kinase inhibitor (oral, cancer), ACT Biotech; Multi-mode kinase inhibitor (oral, cancer), Bayer
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MOA Inhibitor
External Link
 Compound Name PMID20005102C1 Investigative [24]
Synonyms
GTPL8181; BDBM50305878; B99
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MOA Inhibitor
Activity IC50 = 7 nM
External Link
 Compound Name KT-5720 Investigative [25]
Synonyms
KT 5720; KT5720; 108068-98-0; GTPL337; ZINC3873013; KT 5720, &gt; hexyl (15R,16R,18S)-16-hydroxy-15-methyl-3-oxo-28-oxa-4,14,19-triazaoctacyclo[12.11.2.1^{15,18}.0^{2,6}.0^{7,27}.0^{8,13}.0^{19,26}.0^{20,25}]octacosa-1(26),2(6),7(27),8,10,12,20,22,24-nonaene-16-carboxylate; (9S,10S,12R)-2,3,9,10,11,12-Hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3 inverted exclamation marka,2 inverted exclamation marka,1 inverted exclamation marka-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-c
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MOA Inhibitor
External Link
 Compound Name STAUROSPORINONE Investigative [25]
MOA Inhibitor
External Link
 Compound Name Ro31-8220 Investigative [25]
Synonyms
Bisindolylmaleimide IX; ro 31-8220; 125314-64-9; Ro 31 8220; Ro 318220; UNII-W9A0B5E78O; Ro-318220; Ro-31-8220; CHEMBL6291; W9A0B5E78O; CHEBI:38912; 3-{3-[4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indol-1-yl}propyl carbamimidothioate; 3-{3-[4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-2,5-dihydro-1H-pyrrol-3-yl]-1H-indol-1-yl}propyl imidothiocarbamate; CHEMBL1591531; Carbamimidothioic acid, 3-(3-(2,5-dihydro-4-(1-methyl-1H-indol-3-yl)-2,5-dioxo-1H-pyrrol-3-yl)-1H-indol-1-yl)propyl; bisindolymaleimide IX
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MOA Inhibitor
Activity IC50 = 15 nM
External Link
 Compound Name KN-62 Investigative [25]
Synonyms
KN-62 (non-isomeric); GTPL6001; HMS3229A04; CCG-206863
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MOA Inhibitor
External Link
 Compound Name CI-1040 Investigative [25]
MOA Inhibitor
External Link
 Compound Name 4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole Investigative [26]
Synonyms
4,5,6,7-tetrabromobenzotriazole
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MOA Inhibitor
External Link
 Compound Name 4-[(3,5-diamino-1H-pyrazol-4-yl)diazenyl]phenol Investigative [27]
MOA Inhibitor
External Link
 Compound Name RO-316233 Investigative [25]
Synonyms
119139-23-0; bisindolylmaleimide iv; 3,4-di(1H-indol-3-yl)-1H-pyrrole-2,5-dione; Arcyriarubin A; 3,4-Bis(3-indolyl)maleimide; 3,4-Di-1H-indol-3-yl-1H-pyrrole-2,5-dione; UNII-MBK3OO5K8T; BIM IV; 3,4-bis(1H-indol-3-yl)pyrrole-2,5-dione; MBK3OO5K8T; CHEMBL266487; 3,4-bis(1H-indol-3-yl)-2,5-dihydro-1H-pyrrole-2,5-dione; DQYBRTASHMYDJG-UHFFFAOYSA-N; 2,3-bis(1H-Indol-3-yl)maleimide; 1H-Pyrrole-2,5-dione, 3,4-di-1H-indol-3-yl-; Ro-31-6233; AK-15401; 3,4-bis(3-indolyl)-1H-pyrrole-2,5-dione; Bisindoylmaleimide; Bisindolyl deriv. 3
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MOA Inhibitor
External Link
2B72: Gastric cancer 81 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Leniolisib Approved [28]
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
 Compound Name Atezolizumab Approved [5]
External Link
 Compound Name Bavencio Approved [5]
External Link
 Compound Name Tebentafusp Approved [29]
External Link
 Compound Name Merimepodib Approved [30]
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
 Compound Name Taxol Approved [31]
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
 Compound Name Ramucirumab Approved [32]
Synonyms
LY3009806
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External Link
 Compound Name Tucatinib Approved [33]
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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 Compound Name Antacids Approved [34]
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 Compound Name Trastuzumab Approved [5]
Synonyms
Herceptin; Herceptin (TN); Trastuzumab (INN); Trastuzumab (genetical recombination); Trastuzumab (genetical recombination) (JAN); Trastuzumab (ERBB2 mAb inhibitor)
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External Link
 Compound Name Carbamazepine Phase 3 [35]
Synonyms
Carbamazepine (iv, epilepsy); Carbamazepine (iv, epilepsy), Lundbeck; Carbamazepine (iv, epilepsy), Ovation Pharmaceuticals
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External Link
 Compound Name Margetuximab Approved [5]
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 Compound Name Nivolumab Approved [5]
External Link
 Compound Name GRANITE Phase 3 [36]
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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 Compound Name Zolbetuximab Phase 3 [37]
Synonyms
IMAB362
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External Link
 Compound Name Tusamitamab ravtansine Phase 3 [38]
Synonyms
SAR408701
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External Link
 Compound Name Andecaliximab Phase 3 [39]
External Link
 Compound Name ABP 980 Phase 3 [40]
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 Compound Name GS-5745 Phase 3 [31]
External Link
 Compound Name S-1 Phase 3 [41]
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
 Compound Name Lonsurf Phase 3 [5]
External Link
 Compound Name GDC-0068 Phase 3 [31]
Synonyms
RG7440
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External Link
 Compound Name Edotecarin Phase 3 [42]
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
 Compound Name RG3638 Phase 3 [43]
Synonyms
Onartuzumab
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External Link
 Compound Name G17DT Phase 3 [44]
Synonyms
Gastrimmune; Insegia
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External Link
 Compound Name DE-766 Phase 3 [45]
External Link
 Compound Name Tesetaxel Phase 2 [46]
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
 Compound Name Nelipepimut S Phase 3 [47]
Synonyms
E75
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External Link
 Compound Name BMS-986205 Phase 3 [5]
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
 Compound Name Rivoceranib Phase 3 [5]
External Link
 Compound Name Claudiximab Phase 3 [5]
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
 Compound Name OS-440 Phase 3 [48]
Synonyms
CNS modulator (spasticity), Osmotica
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 Compound Name Oraxol Phase 3 [5]
External Link
 Compound Name ICI 118,551 Phase 3 [31]
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
 Compound Name Evorpacept Phase 2/3 [49]
Synonyms
ALX148
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 Compound Name BNT141 Phase 2 [50]
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 Compound Name Anti-LAG3 Phase 2 [40]
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 Compound Name GSK1292263 Phase 2 [51]
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 Compound Name MM-111 Phase 2 [52]
External Link
 Compound Name Plevitrexed Phase 2 [53]
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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External Link
 Compound Name DS-8201 Phase 1 [40]
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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External Link
 Compound Name XL880 Phase 2 [54]
Synonyms
GSK 089; GSK 1363089; GSK1363089; XL 880; GSK1363089, GSK089, foretinib, EXEL-2880, XL880; 88Z; MET inhibitors
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External Link
 Compound Name Matuzumab Phase 2 [55]
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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 Compound Name BAY-57-9352 Phase 2 [31]
Synonyms
Telatinib; Bay 57-9352
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External Link
 Compound Name Bemarituzumab Phase 2 [56]
External Link
 Compound Name PEGPH20 Phase 2 [5]
External Link
 Compound Name Plevitrexed (R)-isomer Phase 2 [57]
Synonyms
YW3548
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 Compound Name APR-246 Phase 2 [58]
Synonyms
Eprenetapopt
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 Compound Name CRS-207 Phase 2 [47]
External Link
 Compound Name Opdivo + Yervoy Phase 3 [5]
External Link
 Compound Name CT-041 Phase 1/2 [59]
External Link
 Compound Name BPX-601 Phase 1/2 [60]
External Link
 Compound Name Anti-MUC1 CAR-T cells Phase 1/2 [61]
External Link
 Compound Name Anti-Mesothelin CAR-T cells Phase 1/2 [62]
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 Compound Name Anti-HER2 CAR-T Phase 1/2 [63]
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 Compound Name CAR-T Cells targeting EpCAM Phase 1/2 [64]
External Link
 Compound Name PAT-SC1 Phase 1/2 [65]
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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 Compound Name ASP2138 Phase 1 [66]
External Link
 Compound Name SAR443216 Phase 1 [67]
External Link
 Compound Name AMG 199 Phase 1 [68]
External Link
 Compound Name AMG 910 Phase 1 [69]
External Link
 Compound Name Alofanib Phase 1 [70]
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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 Compound Name HER2-specific CAR T cell Phase 1 [71]
External Link
 Compound Name Anti-CEA-CAR T Phase 1 [72]
External Link
 Compound Name XR-5944 Phase 1 [73]
Synonyms
MLN-944; XR-11576 analogs; XR-5000 analogs; XR-5942
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External Link
 Compound Name A168 Phase 1 [74]
External Link
 Compound Name EGFR806-specific CAR T cell Phase 1 [75]
External Link
 Compound Name AbGn-107 Phase 1 [5]
External Link
 Compound Name FPA144 Phase 1 [40]
External Link
 Compound Name Minnelide 001 Phase 1 [31]
External Link
 Compound Name CAR-T cells targeting EpCAM Phase 1 [76]
External Link
 Compound Name Anti-CEA CAR-T cells Phase 1 [77]
External Link
 Compound Name EPCAM-targeted CAR-T cells Clinical trial [78]
External Link
 Compound Name PMID28460551-Compound-1 Patented [79]
External Link
 Compound Name Conjugated 3-(indolyl)-and 3-(azaindolyl)-4-arylmaleimide compound 1 Patented [80]
Synonyms
PMID28621580-Compound-WO2012084683c62
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External Link
 Compound Name TOPIXANTRONE HYDROCHLORIDE Discontinued in Phase 2 [81]
Synonyms
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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External Link
 Compound Name MDL 101,731 Discontinued in Phase 2 [82]
Synonyms
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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External Link
 Compound Name BBR-3438 Discontinued in Phase 2 [83]
Synonyms
Nortopixantrone; UNII-PH2639TAB4; PH2639TAB4; Nortopixantrone [INN:BAN]; AC1MI4ZO; CHEMBL150303; SCHEMBL7804438
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External Link
 Compound Name IPI-493 Discontinued in Phase 1 [84]
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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 Compound Name Kanjinti Application submitted [5]
External Link
 Compound Name Anti-CD9 mab Investigative [85]
Synonyms
ALB-6; Anti-CD9 mAb (gastric cancer); Anti-CD9 mAb (gastric cancer), Osaka University
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External Link
References
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