m6A-centered Crosstalk Information

Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT03635
 [1], [2]
Histone modification H3K27me3 EZH2 miR-338-5p Indirect Enhancement m6A modification BAX BAX METTL3 Methylation : m6A sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
 Regulator Info 
m6A Target Apoptosis regulator BAX (BAX)
 Targert Gene 
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 Apoptosis regulator BAX (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
 Disease Info 
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 BAX (BAX) 1 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Thymoquinone Phase 2/3 [3]
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
CID: 10281
TTD: DY4OZ6
Histone-lysine N-methyltransferase EZH2 (EZH2) 74 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Tazemetostat Approved [4]
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
CID: 66558664
TTD: D00EQL
DrugBank: DB12887
 Compound Name DS-3201b Phase 2 [5]
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
External Link
CID: 126481870
TTD: DNM79H
 Compound Name CPI-1205 Phase 1/2 [6]
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
CID: 78320408
TTD: D0E6AG
DrugBank: DB14581
 Compound Name SHR2554 Phase 1/2 [7]
MOA Inhibitor
External Link
TTD: DM5X0L
 Compound Name CPI-0209 Phase 1/2 [8]
MOA Inhibitor
External Link
TTD: DXL38G
 Compound Name GSK2816126 Phase 1 [9]
Synonyms
GSK 126; GSK-126
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MOA Modulator
Activity Ki = 0.5 nM
External Link
CID: 68210102
TTD: D05FIJ
 Compound Name PF-06821497 Phase 1 [10]
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
External Link
CID: 118572065
TTD: DI1L7M
DrugBank: DB14799
 Compound Name DS-3201 Phase 1 [6]
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
CID: 22627096
TTD: D0LG8T
 Compound Name HH2853 Phase 1 [11]
MOA Inhibitor
External Link
TTD: D6EU7R
 Compound Name PMID28394193-Compound-33 Patented [12]
MOA Inhibitor
Activity IC50 = 100 nM
External Link
CID: 121305270
TTD: D03MYI
 Compound Name PMID28394193-Compound-Figure3bI Patented [12]
MOA Inhibitor
External Link
TTD: D04PCW
 Compound Name PMID28394193-Compound-35 Patented [12]
MOA Inhibitor
Activity IC50 = 10 nM
External Link
TTD: D05MAR
 Compound Name PMID28394193-Compound-54 Patented [12]
MOA Inhibitor
External Link
TTD: D07CZI
 Compound Name PMID28394193-Compound-24 Patented [12]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
CID: 117807842
TTD: D08MXO
 Compound Name PMID28394193-Compound-27 Patented [12]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
CID: 76684269
TTD: D09GFF
 Compound Name PMID28394193-Compound-25 Patented [12]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
CID: 117807842
TTD: D09PQQ
 Compound Name PMID28394193-Compound-50 Patented [12]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
CID: 118580552
TTD: D0A0VH
 Compound Name PMID28394193-Compound-47 Patented [12]
MOA Inhibitor
Activity IC50 = 2 nM; Ki < 1 nM
External Link
CID: 118616529
TTD: D0B4TX
 Compound Name PMID28394193-Compound-21 Patented [12]
MOA Inhibitor
External Link
TTD: D0BL8W
 Compound Name PMID28394193-Compound-41 Patented [12]
MOA Inhibitor
External Link
CID: 118101320
TTD: D0BT6Y
 Compound Name PMID28394193-Compound-53 Patented [12]
MOA Inhibitor
Activity IC50 = 80 nM
External Link
CID: 121322599
TTD: D0CH4O
 Compound Name PMID28394193-Compound-Figure5aVIII Patented [12]
MOA Inhibitor
External Link
TTD: D0D1QD
 Compound Name PMID28394193-Compound-38 Patented [12]
MOA Inhibitor
External Link
CID: 78320108
TTD: D0DQ6N
 Compound Name PMID28394193-Compound-51 Patented [12]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
CID: 118580509
TTD: D0FC9J
 Compound Name PMID28394193-Compound-31 Patented [12]
MOA Inhibitor
Activity IC50 = 20 nM
External Link
TTD: D0FI3A
 Compound Name PMID28394193-Compound-42 Patented [12]
MOA Inhibitor
External Link
CID: 118096643
TTD: D0H4HR
 Compound Name PMID28394193-Compound-15 Patented [12]
MOA Inhibitor
External Link
TTD: D0KR2T
 Compound Name PMID28394193-Compound-52 Patented [12]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
CID: 118580510
TTD: D0LR5O
 Compound Name PMID28394193-Compound-32 Patented [12]
MOA Inhibitor
Activity IC50 = 500 nM
External Link
TTD: D0M1TG
 Compound Name PMID28394193-Compound-23 Patented [12]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
CID: 117807623
TTD: D0M9BY
 Compound Name PMID28394193-Compound-29 Patented [12]
MOA Inhibitor
Activity IC50 = 100 nM
External Link
TTD: D0MH8G
 Compound Name PMID28394193-Compound-30 Patented [12]
MOA Inhibitor
Activity IC50 = 16 nM
External Link
TTD: D0MO2X
 Compound Name PMID28394193-Compound-39 Patented [12]
MOA Inhibitor
External Link
TTD: D0MZ8D
 Compound Name PMID28394193-Compound-49 Patented [12]
MOA Inhibitor
Activity IC50 > 1 nM; IC50 < 2 nM; Ki > 0.01 nM; Ki < 0.04 nM
External Link
CID: 118572078
TTD: D0PB6T
 Compound Name PMID28394193-Compound-43 Patented [12]
MOA Inhibitor
External Link
CID: 118096796
TTD: D0PI5O
 Compound Name PMID28394193-Compound-40 Patented [12]
MOA Inhibitor
External Link
CID: 118095598
TTD: D0QH1J
 Compound Name PMID28394193-Compound-Figure3bIII Patented [12]
MOA Inhibitor
External Link
TTD: D0R2TQ
 Compound Name PMID28394193-Compound-36 Patented [12]
MOA Inhibitor
Activity IC50 = 316 nM
External Link
TTD: D0RD5P
 Compound Name PMID28394193-Compound-28 Patented [12]
MOA Inhibitor
Activity IC50 = 32 nM
External Link
CID: 91884579
TTD: D0S4OP
 Compound Name PMID28394193-Compound-22 Patented [12]
MOA Inhibitor
External Link
TTD: D0SQ1R
 Compound Name PMID28394193-Compound-18 Patented [12]
MOA Inhibitor
External Link
TTD: D0SY6P
 Compound Name PMID28394193-Compound-16 Patented [12]
MOA Inhibitor
External Link
TTD: D0T8QL
 Compound Name PMID28394193-Compound-44 Patented [12]
MOA Inhibitor
External Link
CID: 118096614
TTD: D0U9OH
 Compound Name PMID28394193-Compound-20 Patented [12]
MOA Inhibitor
External Link
TTD: D0UG5O
 Compound Name PMID28394193-Compound-19 Patented [12]
MOA Inhibitor
External Link
TTD: D0VF0M
 Compound Name PMID28394193-Compound-37 Patented [12]
MOA Inhibitor
External Link
CID: 78320107
TTD: D0W2KL
 Compound Name PMID28394193-Compound-Figure3bII Patented [12]
MOA Inhibitor
External Link
TTD: D0W4MW
 Compound Name PMID28394193-Compound-26 Patented [12]
MOA Inhibitor
Activity IC50 < 1000 nM
External Link
CID: 75203283
TTD: D0Z0NC
 Compound Name PMID28394193-Compound-17 Patented [12]
MOA Inhibitor
External Link
TTD: D0Z0QS
 Compound Name PMID28394193-Compound-34 Patented [12]
MOA Inhibitor
Activity IC50 = 100 nM
External Link
TTD: D0Z7GN
 Compound Name PMID28394193-Compound-56 Patented [12]
MOA Inhibitor
Activity IC50 = 0.93 nM
External Link
TTD: D01PZZ
 Compound Name PMID28394193-Compound-46 Patented [12]
MOA Inhibitor
Activity IC50 = 5 nM
External Link
CID: 102593999
TTD: D0D4UH
 Compound Name PMID28394193-Compound-57 Patented [12]
MOA Inhibitor
Activity IC50 = 6.45 nM
External Link
TTD: D0G1JR
 Compound Name PMID28394193-Compound-14 Patented [12]
MOA Inhibitor
Activity IC50 = 21900 nM
External Link
CID: 90467336
TTD: D0GT7A
 Compound Name PMID28394193-Compound-12 Patented [12]
MOA Inhibitor
Activity IC50 < 10 nM
External Link
TTD: D0H8VN
 Compound Name PMID26882240-Compound-1 Patented [13]
MOA Inhibitor
External Link
CID: 5712
TTD: D0L1TA
 Compound Name PMID28394193-Compound-55 Patented [12]
MOA Inhibitor
Activity IC50 = 8.13 nM
External Link
TTD: D0M4LK
 Compound Name PMID28394193-Compound-45 Patented [12]
MOA Inhibitor
Activity IC50 = 168000 nM
External Link
CID: 118607675
TTD: D0M8AA
 Compound Name PMID28394193-Compound-13 Patented [12]
MOA Inhibitor
Activity IC50 = 1470 nM
External Link
CID: 86765324
TTD: D0TA4N
 Compound Name EPZ005687 Investigative [14]
Synonyms
EPZ-005687; EPZ 005687
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MOA Inhibitor
External Link
CID: 60160561
TTD: D02BBA
 Compound Name EI1 Investigative [15]
Synonyms
KB-145943
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MOA Inhibitor
External Link
CID: 72199293
TTD: D02CIT
 Compound Name UNC1999 Investigative [16]
Synonyms
UNC 1999; UNC-1999
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MOA Inhibitor
External Link
CID: 72551585
TTD: D02YXP
 Compound Name MS1943 Investigative [7]
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
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MOA Degrader
External Link
CID: 139211327
TTD: D65IMT
 Compound Name GSK343 Investigative [17]
Synonyms
compound 6 [PMID 24900432]; GSK 343
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 174 nM
External Link
CID: 71268957
TTD: D02TVQ
 Compound Name PMID28394193-Compound-11 Patented [18]
External Link
TTD: D0MH5C
 Compound Name PMID28394193-Compound-10 Patented [18]
External Link
TTD: D0MZ9P
 Compound Name PMID28394193-Compound-14 Patented [12]
MOA Inhibitor
Activity IC50 = 21900 nM
External Link
CID: 90467336
TTD: D0GT7A
 Compound Name PMID28394193-Compound-12 Patented [12]
MOA Inhibitor
Activity IC50 < 10 nM
External Link
TTD: D0H8VN
 Compound Name PMID28394193-Compound-13 Patented [12]
MOA Inhibitor
Activity IC50 = 1470 nM
External Link
CID: 86765324
TTD: D0TA4N
 Compound Name PMID28394193-Compound-56 Patented [12]
MOA Inhibitor
Activity IC50 = 0.93 nM
External Link
TTD: D01PZZ
 Compound Name PMID28394193-Compound-46 Patented [12]
MOA Inhibitor
Activity IC50 = 5 nM
External Link
CID: 102593999
TTD: D0D4UH
 Compound Name PMID28394193-Compound-57 Patented [12]
MOA Inhibitor
Activity IC50 = 6.45 nM
External Link
TTD: D0G1JR
 Compound Name PMID28394193-Compound-55 Patented [12]
MOA Inhibitor
Activity IC50 = 8.13 nM
External Link
TTD: D0M4LK
 Compound Name PMID28394193-Compound-45 Patented [12]
MOA Inhibitor
Activity IC50 = 168000 nM
External Link
CID: 118607675
TTD: D0M8AA
2B72: Gastric cancer 81 Compound(s) Regulating the Disease Click to Show/Hide the Full List
 Compound Name Leniolisib Approved [19]
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
    Click to Show/Hide
External Link
CID: 57495353
TTD: DGO2C1
 Compound Name Atezolizumab Approved [6]
External Link
TTD: D0YM2K
 Compound Name Bavencio Approved [6]
External Link
TTD: D0W8HN
 Compound Name Tebentafusp Approved [20]
External Link
TTD: D0S0BJ
 Compound Name Merimepodib Approved [21]
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
CID: 153241
TTD: D0F0ZE
DrugBank: DB04862
 Compound Name Taxol Approved [22]
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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CID: 36314
TTD: D0C4RB
DrugBank: DB01229
 Compound Name Ramucirumab Approved [23]
Synonyms
LY3009806
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TTD: D09HVD
 Compound Name Tucatinib Approved [24]
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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CID: 51039094
TTD: D09GRX
DrugBank: DB11652
 Compound Name Antacids Approved [25]
External Link
TTD: D06AJL
 Compound Name Trastuzumab Approved [6]
Synonyms
Herceptin; Herceptin (TN); Trastuzumab (INN); Trastuzumab (genetical recombination); Trastuzumab (genetical recombination) (JAN); Trastuzumab (ERBB2 mAb inhibitor)
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TTD: D04WFL
 Compound Name Carbamazepine Phase 3 [26]
Synonyms
Carbamazepine (iv, epilepsy); Carbamazepine (iv, epilepsy), Lundbeck; Carbamazepine (iv, epilepsy), Ovation Pharmaceuticals
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External Link
CID: 2554
TTD: D04MSM
DrugBank: DB00564
 Compound Name Margetuximab Approved [6]
External Link
TTD: D01YYP
 Compound Name Nivolumab Approved [6]
External Link
TTD: D00GOV
 Compound Name GRANITE Phase 3 [27]
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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CID: 11784975
TTD: DKF9I3
 Compound Name Zolbetuximab Phase 3 [28]
Synonyms
IMAB362
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External Link
TTD: D4HQ1F
 Compound Name Tusamitamab ravtansine Phase 3 [29]
Synonyms
SAR408701
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External Link
TTD: D2D6NJ
 Compound Name Andecaliximab Phase 3 [30]
External Link
TTD: D0Z6SP
 Compound Name ABP 980 Phase 3 [31]
External Link
TTD: D0WZ0X
 Compound Name GS-5745 Phase 3 [22]
External Link
CID: 56776542
TTD: D0WL0Q
 Compound Name S-1 Phase 3 [32]
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
CID: 163872
TTD: D0S8LJ
 Compound Name Lonsurf Phase 3 [6]
External Link
TTD: D0PM0Y
 Compound Name GDC-0068 Phase 3 [22]
Synonyms
RG7440
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External Link
CID: 24788740
TTD: D0I4TH
DrugBank: DB11743
 Compound Name Edotecarin Phase 3 [33]
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
    Click to Show/Hide
External Link
CID: 9808998
TTD: D0I1DW
DrugBank: DB04882
 Compound Name RG3638 Phase 3 [34]
Synonyms
Onartuzumab
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External Link
TTD: D0H9PT
 Compound Name G17DT Phase 3 [35]
Synonyms
Gastrimmune; Insegia
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External Link
TTD: D0G8ZQ
 Compound Name DE-766 Phase 3 [36]
External Link
TTD: D0FJ1W
 Compound Name Tesetaxel Phase 2 [37]
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
CID: 6918574
TTD: D0F9VH
DrugBank: DB12019
 Compound Name Nelipepimut S Phase 3 [38]
Synonyms
E75
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External Link
CID: 9941306
TTD: D0F8UV
 Compound Name BMS-986205 Phase 3 [6]
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
CID: 121328278
TTD: D0DP5I
DrugBank: DB14986
 Compound Name Rivoceranib Phase 3 [6]
External Link
TTD: D0D7BX
 Compound Name Claudiximab Phase 3 [6]
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
TTD: D0B3ZC
 Compound Name OS-440 Phase 3 [39]
Synonyms
CNS modulator (spasticity), Osmotica
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External Link
TTD: D09OHH
 Compound Name Oraxol Phase 3 [6]
External Link
TTD: D04UWU
 Compound Name ICI 118,551 Phase 3 [22]
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
CID: 3682
TTD: D04DJS
 Compound Name Evorpacept Phase 2/3 [40]
Synonyms
ALX148
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TTD: DRP8H0
 Compound Name BNT141 Phase 2 [41]
External Link
TTD: DFZ19J
 Compound Name Anti-LAG3 Phase 2 [31]
External Link
TTD: D0T7OI
 Compound Name GSK1292263 Phase 2 [42]
External Link
CID: 24996872
TTD: D0S4II
DrugBank: DB12627
 Compound Name MM-111 Phase 2 [43]
External Link
TTD: D0Q2KM
 Compound Name Plevitrexed Phase 2 [44]
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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CID: 135430970
TTD: D0I9GR
DrugBank: DB06163
 Compound Name DS-8201 Phase 1 [31]
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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CID: 10671
TTD: D0E8IQ
 Compound Name XL880 Phase 2 [45]
Synonyms
GSK 089; GSK 1363089; GSK1363089; XL 880; GSK1363089, GSK089, foretinib, EXEL-2880, XL880; 88Z; MET inhibitors
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External Link
CID: 42642645
TTD: D0D1GF
DrugBank: DB12307
 Compound Name Matuzumab Phase 2 [46]
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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External Link
TTD: D0BZ7V
 Compound Name BAY-57-9352 Phase 2 [22]
Synonyms
Telatinib; Bay 57-9352
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External Link
CID: 9808844
TTD: D07NOI
DrugBank: DB15393
 Compound Name Bemarituzumab Phase 2 [47]
External Link
TTD: D05ISO
 Compound Name PEGPH20 Phase 2 [6]
External Link
TTD: D05INV
 Compound Name Plevitrexed (R)-isomer Phase 2 [48]
Synonyms
YW3548
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External Link
CID: 213022
TTD: D04FYZ
 Compound Name APR-246 Phase 2 [49]
Synonyms
Eprenetapopt
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External Link
CID: 52918385
TTD: D03XTY
DrugBank: DB11684
 Compound Name CRS-207 Phase 2 [38]
External Link
TTD: D02WSB
 Compound Name Opdivo + Yervoy Phase 3 [6]
External Link
TTD: D02VYE
 Compound Name CT-041 Phase 1/2 [50]
External Link
TTD: DJ6AW5
 Compound Name BPX-601 Phase 1/2 [51]
External Link
TTD: D0TY6U
 Compound Name Anti-MUC1 CAR-T cells Phase 1/2 [52]
External Link
TTD: D0C9MJ
 Compound Name Anti-Mesothelin CAR-T cells Phase 1/2 [53]
External Link
TTD: D0BE6M
 Compound Name Anti-HER2 CAR-T Phase 1/2 [54]
External Link
TTD: D08QZH
 Compound Name CAR-T Cells targeting EpCAM Phase 1/2 [55]
External Link
TTD: D08QYW
 Compound Name PAT-SC1 Phase 1/2 [56]
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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TTD: D00UOQ
 Compound Name ASP2138 Phase 1 [57]
External Link
TTD: DTQL30
 Compound Name SAR443216 Phase 1 [58]
External Link
TTD: DL6F3E
 Compound Name AMG 199 Phase 1 [59]
External Link
TTD: DEP3Z8
 Compound Name AMG 910 Phase 1 [60]
External Link
TTD: DEDP81
 Compound Name Alofanib Phase 1 [61]
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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External Link
CID: 86280646
TTD: D47MOS
 Compound Name HER2-specific CAR T cell Phase 1 [62]
External Link
TTD: D0YF6K
 Compound Name Anti-CEA-CAR T Phase 1 [63]
External Link
TTD: D0S1QN
 Compound Name XR-5944 Phase 1 [64]
Synonyms
MLN-944; XR-11576 analogs; XR-5000 analogs; XR-5942
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External Link
CID: 439035
TTD: D0Q5TH
DrugBank: DB06364
 Compound Name A168 Phase 1 [65]
External Link
TTD: D0L9PU
 Compound Name EGFR806-specific CAR T cell Phase 1 [66]
External Link
TTD: D0I7ZH
 Compound Name AbGn-107 Phase 1 [6]
External Link
TTD: D08GZE
 Compound Name FPA144 Phase 1 [31]
External Link
TTD: D06NND
 Compound Name Minnelide 001 Phase 1 [22]
External Link
TTD: D05UFJ
 Compound Name CAR-T cells targeting EpCAM Phase 1 [67]
External Link
TTD: D01TNK
 Compound Name Anti-CEA CAR-T cells Phase 1 [68]
External Link
TTD: D00KDQ
 Compound Name EPCAM-targeted CAR-T cells Clinical trial [69]
External Link
TTD: D0T8DD
 Compound Name PMID28460551-Compound-1 Patented [70]
External Link
CID: 25190990
TTD: D0IH3I
DrugBank: DB14866
 Compound Name Conjugated 3-(indolyl)-and 3-(azaindolyl)-4-arylmaleimide compound 1 Patented [71]
Synonyms
PMID28621580-Compound-WO2012084683c62
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External Link
TTD: D04PKQ
 Compound Name TOPIXANTRONE HYDROCHLORIDE Discontinued in Phase 2 [72]
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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CID: 6918273
TTD: D06DWQ
 Compound Name MDL 101,731 Discontinued in Phase 2 [73]
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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CID: 6435808
TTD: D05HZI
DrugBank: DB06433
 Compound Name BBR-3438 Discontinued in Phase 2 [74]
Synonyms
Nortopixantrone; UNII-PH2639TAB4; PH2639TAB4; Nortopixantrone [INN:BAN]; AC1MI4ZO; CHEMBL150303; SCHEMBL7804438
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CID: 3038512
TTD: D01VPR
 Compound Name IPI-493 Discontinued in Phase 1 [75]
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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External Link
CID: 9893658
TTD: D0BM6S
DrugBank: DB13023
 Compound Name Kanjinti Application submitted [6]
External Link
TTD: D0CW3U
 Compound Name Anti-CD9 mab Investigative [76]
Synonyms
ALB-6; Anti-CD9 mAb (gastric cancer); Anti-CD9 mAb (gastric cancer), Osaka University
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External Link
TTD: D09BPT
References
Ref 1 Methylation of microRNA-338-5p by EED promotes METTL3-mediated translation of oncogene CDCP1 in gastric cancer. Aging (Albany NY). 2021 Apr 21;13(8):12224-12238. doi: 10.18632/aging.103822. Epub 2021 Apr 21.
Ref 2 METTL3 Promotes the Proliferation and Mobility of Gastric Cancer Cells. Open Med (Wars). 2019 Mar 2;14:25-31. doi: 10.1515/med-2019-0005. eCollection 2019.
Ref 3 Apoptosis as a mechanism for the treatment of adult T cell leukemia: promising drugs from benchside to bedside. Drug Discov Today. 2020 Jul;25(7):1189-1197. doi: 10.1016/j.drudis.2020.04.023. Epub 2020 May 7.
Ref 4 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
Ref 5 Development of new agents for peripheral T-cell lymphoma. Expert Opin Biol Ther. 2019 Mar;19(3):197-209. doi: 10.1080/14712598.2019.1572746. Epub 2019 Jan 29.
Ref 6 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 7 Epigenetics and beyond: targeting writers of protein lysine methylation to treat disease. Nat Rev Drug Discov. 2021 Apr;20(4):265-286. doi: 10.1038/s41573-020-00108-x. Epub 2021 Jan 19.
Ref 8 ClinicalTrials.gov (NCT04104776) A Study of CPI-0209 in Patients With Advanced Tumors. U.S. National Institutes of Health.
Ref 9 National Cancer Institute Drug Dictionary (drug id 756211).
Ref 10 Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497). J Med Chem. 2018 Feb 8;61(3):650-665. doi: 10.1021/acs.jmedchem.7b01375. Epub 2017 Dec 27.
Ref 11 Clinical pipeline report, company report or official report of HaiHe Biopharma.
Ref 12 EZH2 inhibitors: a patent review (2014-2016). Expert Opin Ther Pat. 2017 Jul;27(7):797-813. doi: 10.1080/13543776.2017.1316976. Epub 2017 Apr 20.
Ref 13 Hypoxia-inducible factor (HIF) inhibitors: a patent survey (2011-2015). Expert Opin Ther Pat. 2016;26(3):309-22. doi: 10.1517/13543776.2016.1146252. Epub 2016 Feb 16.
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