Mechanism of Crosstalk between m6A Modification and Epigenetic Regulation
Crosstalk ID
M6ACROT03656
[1], [2]
Histone modification H3K27me3 EZH2 miR-338-5p Indirect Enhancement m6A modification PARP1 PARP1 METTL3 Methylation : m6A sites
m6A Modification:
m6A Regulator Methyltransferase-like 3 (METTL3) WRITER
m6A Target Poly [ADP-ribose] polymerase 1 (PARP1)
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. m6A methyltransferase METTL3 facilitates oxaliplatin resistance in CD133+ gastric cancer stem cells by Promoting Poly [ADP-ribose] polymerase 1 (PARP1) mRNA stability which increases base excision repair pathway activity. METTTL3 enhances the stability of PARP1 by recruiting YTHDF1 to target the 3'-untranslated Region (3'-UTR) of PARP1 mRNA.
Responsed Disease Gastric cancer ICD-11: 2B72
Responsed Drug Oxaliplatin
Pathway Response Nucleotide excision repair hsa03420
Signaling pathways regulating pluripotency of stem cells hsa04550
Cell Process RNA stability
Excision repair
In-vitro Model
MKN74 Gastric tubular adenocarcinoma Homo sapiens CVCL_2791
HEK293T Normal Homo sapiens CVCL_0063
AGS Gastric adenocarcinoma Homo sapiens CVCL_0139
SNU-719 Gastric tubular adenocarcinoma Homo sapiens CVCL_5086
In-vivo Model 100,000 pLKO and PARP1-sh1 (PT1 and PT2) cells were mixed with matrix gel and inoculate into BALB/C nude mice, respectively. After 25 days, 6 organoid transplanted tumor mice were treated with oxaliplatin (Sellekchem, s1224) twice a week for 4 weeks at a dose of 5 mg/kg.
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
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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
    Click to Show/Hide
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
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name EI1 Investigative [14]
Synonyms
KB-145943
    Click to Show/Hide
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
    Click to Show/Hide
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
Poly [ADP-ribose] polymerase 1 (PARP1) 131 Compound(s) Regulating the Target Click to Show/Hide the Full List
 Compound Name Nicotinamide Approved [18]
Synonyms
Aminicotin; Amixicotyn; Amnicotin; Benicot; Dipegyl; Endobion; Enduramide; Hansamid; Mediatric; Niacevit; Niacinamide; Niacotinamide; Niamide; Nicamina; Nicamindon; Nicasir; Nicobion; Nicofort; Nicogen; Nicomidol; Nicosylamide; Nicota; Nicotamide; Nicotilamide; Nicotililamido; Nicotinamid; Nicotinamida; Nicotinamidum; Nicotinsaeureamid; Nicotinsaureamid; Nicotol; Nicotylamide; Nicotylamidum; Nicovit; Nicovitina; Nicovitol; Nicozymin; Nikasan; Nikazan; Nikotinamid; Nikotinsaeureamid; Niocinamide; Niozymin; Papulex; Pelmin; Pelmine; Savacotyl; Amid kyseliny nikotinove; Amid kyseliny nikotinove [Czech]; Amide PP; Astra Brand of Niacinamide; Austrovit PP; Delonin amide; Factor pp; Inovitan PP; Jenapharm Brand of Niacinamide; Merck Brand of Niacinamide; Niacinamide Astra Brand; Niacinamide Jenapharm Brand; Niacinamide Merck Brand; Niacinamide Pharmagenix Brand; Niacinamide [USAN]; Niavit PP; Nicotine acid amide; Nicotine amide; Nicotinic acid amide; Nicotinic amide; Nicotinsaureamid Jenapharm; Nicotinsaureamid [German]; Nikotinsaeureamid [German]; Pelonin amide; Pharmagenix Brand of Niacinamide; Vitamin B; Vitamin PP; Witamina PP; Nicosan 2; Vitamin H1; B 3, Vitamin; B3, Vitamin; Beta-Pyridinecarboxamide; Jenapharm, Nicotinsaureamid; Nandervit-N; Niacin-Vitamin B3; Niacinamide (USP); Nicotinamida [INN-Spanish]; Nicotinamide (Niacinamide); Nicotinamidum [INN-Latin]; Niko-tamin; PP-Faktor; Vi-Nicotyl; Vitamin B (VAN); M-(Aminocarbonyl)pyridine; Niacinamide, Nicotinic acid amide, Nicotinamide; Nicotinamide (JP15/INN); Nicotinamide, niacin, vitamin B3; Nicotinamide-carbonyl-14C; Pyridine-3-carboxamide; Pyridine-3-carboxylic acid amide; 3 Pyridinecarboxamide; 3-Carbamoylpyridine; 3-Pyridinecarboxamide; 3-Pyridinecarboxylic acid amide
    Click to Show/Hide
MOA Binder
Activity IC50 = 210000 nM
External Link
 Compound Name KU-0058948 Approved [19]
Synonyms
CHEMBL380648; 4-[3-(1,4-diazepan-1-ylcarbonyl)-4-fluorobenzyl]phthalazin-1(2H)-one; 4-(3-(1,4-diazepane-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one; Homopiperazine analogue, 14; SCHEMBL864319; BDBM27533; HGEPGGJUGUMFHT-UHFFFAOYSA-N; ZINC3821234; DB08058; NCGC00386677-01; KU-58948; FT-0670691; TL80090044; 4-[3-([1,4]diazepane-1-carbonyl)-4 -fluorobenzyl]-2H-phthalazin-1-one; 4-[3-([1,4]diazepane-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 7 nM
External Link
 Compound Name Niraparib Tosylate Approved [20]
Synonyms
1038915-73-9; MK-4827 (tosylate); MK-4827 tosylate; UNII-75KE12AY9U; MK-4827(Niraparib) tosylate; 75KE12AY9U; MK-4827-tosylate; MK 4827 tosylate; Niraparib(MK-4827) tosylate; KS-00000TSH; MolPort-044-556-849; s7625; HY-10619B; AKOS030632785; CS-2283; AC-30383; KB-335358; AX8326059
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MOA Modulator
External Link
 Compound Name Nicaraven Phase 3 [21]
Synonyms
AVS; Antevan; Antevas
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MOA Modulator
External Link
 Compound Name CC-486 Phase 3 [22]
Synonyms
AG-14361; AG14361; 328543-09-5; UNII-48N0U0K50I; AG 14361; CHEMBL65892; 48N0U0K50I; Imidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one, 2-[4-[(dimethylamino)methyl]phenyl]-5,6-dihydro-; AG-014361; 1-(4-((dimethylamino)methyl)phenyl)-8,9-dihydro-2,7,9a-triazabenzo[cd]azulen-6(7H)-one; Imidazo(4,5,1-jk)(1,4)benzodiazepin-7(4H)-one, 2-(4-((dimethylamino)methyl)phenyl)-5,6-dihydro-; 2-[4-[(Dimethylamino)methyl]phenyl]-5,6-dihydroimidazo[4,5,1-jk][1,4]benzodiazepin-7(4H)-one; SMR000486393; MLS006011157; MLS001065917; Nucleoside analogue
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MOA Inhibitor
Activity Ki = 5.8 nM
External Link
 Compound Name AG140699 Phase 2 [23]
MOA Inhibitor
External Link
 Compound Name AZD5305 Phase 2 [24]
Synonyms
16MZ1V3RBT; 2589531-76-8; 2-Pyridinecarboxamide, 5-(4-((7-ethyl-5,6-dihydro-6-oxo-1,5-naphthyridin-3-yl)methyl)-1-piperazinyl)-N-methyl-; 2-Pyridinecarboxamide, 5-[4-[(7-ethyl-5,6-dihydro-6-oxo-1,5-naphthyridin-3-yl)methyl]-1-piperazinyl]-N-methyl-; 5-(4-((7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl)piperazin-1-yl)-N-methylpicolinamide; 5-[4-[(7-Ethyl-6-oxo-5,6-dihydro-1,5-naphthyridin-3-yl)methyl]-1-piperazinyl]-N-methylpicolinamide; 5-[4-[(7-ethyl-6-oxo-5H-1,5-naphthyridin-3-yl)methyl]piperazin-1-yl]-N-methylpyridine-2-carboxamide; 5-{4-[(7-ethyl-5,6-dihydro-6-oxo-1,5-naphthyridin-3- yl)methyl]piperazin-1-yl}-N-methylpyridine-2- carboxamide; AC-37130; Azd 5305; AZD 5305 [WHO-DD]; AZD5305; AZD-5305; AZD-5305 [WHO-DD]; CHEMBL5095220; CS-0163534; E80364; EX-A5234; example 4 [WO2021013735]; GTPL11526; HY-132167; MS-26971; NSC834196; NSC-834196; Saruparib; saruparib [INN]; SCHEMBL22912701; SY295016; UNII-16MZ1V3RBT
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MOA Inhibitor
External Link
 Compound Name PMID27841036-Compound-37 Phase 2 [25]
Synonyms
2X-121
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MOA Inhibitor
Activity IC50 = 2 nM
External Link
 Compound Name Stenoparib Phase 2 [26]
MOA Inhibitor
External Link
 Compound Name AMXI 5001 Phase 1/2 [27]
MOA Inhibitor
External Link
 Compound Name NMS-03305293 Phase 1 [28]
Synonyms
NMS-P293
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MOA Inhibitor
External Link
 Compound Name 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 1 Patented [25]
Synonyms
PMID27841036-Compound-6
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MOA Inhibitor
Activity IC50 = 230 nM
External Link
 Compound Name Benzimidazole carboxamide derivative 1 Patented [25]
Synonyms
PMID27841036-Compound-I
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MOA Inhibitor
Activity IC50 < 1 nM
External Link
 Compound Name PMID27841036-Compound-33 Patented [25]
MOA Inhibitor
Activity IC50 = 10 nM
External Link
 Compound Name 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 4 Patented [25]
Synonyms
PMID27841036-Compound-9
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MOA Inhibitor
Activity IC50 = 44 nM
External Link
 Compound Name Phthalazine ketone derivative 1 Patented [25]
Synonyms
PMID27841036-Compound-16
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MOA Inhibitor
Activity IC50 = 6000 nM
External Link
 Compound Name Quinazolinedione derivative 3 Patented [25]
Synonyms
PMID27841036-Compound-13
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MOA Inhibitor
Activity IC50 = 140 nM
External Link
 Compound Name 4-Carboxamido-isoindolinone derivative 2 Patented [25]
Synonyms
PMID27841036-Compound-3
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MOA Inhibitor
Activity IC50 = 11 nM
External Link
 Compound Name 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 3 Patented [25]
Synonyms
PMID27841036-Compound-8
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MOA Inhibitor
Activity IC50 = 15 nM; Kd < 10 nM
External Link
 Compound Name 7-azaindole derivative 8 Patented [25]
Synonyms
PMID27841036-Compound-10
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MOA Inhibitor
Activity IC50 < 100 nM
External Link
 Compound Name 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 5 Patented [25]
Synonyms
PMID27841036-Compound-IV
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MOA Inhibitor
External Link
 Compound Name Phthalazine ketone derivative 3 Patented [25]
Synonyms
PMID27841036-Compound-18
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MOA Inhibitor
Activity IC50 = 9000 nM
External Link
 Compound Name Dihydropyrido phthalazinone derivative 1 Patented [25]
Synonyms
PMID27841036-Compound-21
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MOA Inhibitor
Activity IC50 < 800 nM
External Link
 Compound Name Phthalazine ketone derivative 2 Patented [25]
Synonyms
PMID27841036-Compound-17
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MOA Inhibitor
Activity IC50 = 8000 nM
External Link
 Compound Name Tricyclic indole compound 13 Patented [25]
Synonyms
PMID27841036-Compound-XVI
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MOA Inhibitor
Activity IC50 = 10 to 270 nM
External Link
 Compound Name 3-phenyl isoquinolin-1(2H) derivative 2 Patented [25]
Synonyms
PMID27841036-Compound-VII
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MOA Inhibitor
External Link
 Compound Name 4-Carboxamido-isoindolinone derivative 5 Patented [25]
Synonyms
PMID27841036-Compound-III
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MOA Inhibitor
External Link
 Compound Name Quinazolinedione derivative 2 Patented [25]
Synonyms
PMID27841036-Compound-12
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MOA Inhibitor
Activity IC50 = 0.37 nM
External Link
 Compound Name Quinazolinedione derivative 1 Patented [25]
Synonyms
PMID27841036-Compound-11
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MOA Inhibitor
Activity IC50 = 0.21 nM
External Link
 Compound Name Dihydropyrido phthalazinone derivative 2 Patented [25]
Synonyms
PMID27841036-Compound-22
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MOA Inhibitor
Activity IC50 < 800 nM
External Link
 Compound Name 3-oxo-2,3-dihydro-1H-indazole-4-carboxamide derivative 2 Patented [25]
Synonyms
PMID27841036-Compound-7
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MOA Inhibitor
Activity IC50 = 26 nM; Kd < 10 nM
External Link
 Compound Name Phthalazine derivative 3 Patented [25]
Synonyms
PMID27841036-Compound-19
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MOA Inhibitor
Activity IC50 = 10 nM
External Link
 Compound Name Tetra-hydro-quinoline derivative 1 Patented [25]
Synonyms
PMID27841036-Compound-VIII
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MOA Inhibitor
Activity IC50 = 1 to 500 nM
External Link
 Compound Name 4-Carboxamido-isoindolinone derivative 1 Patented [25]
Synonyms
PMID27841036-Compound-2
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MOA Inhibitor
Activity IC50 = 20 nM
External Link
 Compound Name 4-Carboxamido-isoindolinone derivative 3 Patented [25]
Synonyms
PMID27841036-Compound-4
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MOA Inhibitor
Activity IC50 = 100 nM
External Link
 Compound Name 4-Carboxamido-isoindolinone derivative 4 Patented [25]
Synonyms
PMID27841036-Compound-5
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MOA Inhibitor
Activity IC50 = 20 nM
External Link
 Compound Name Dihydrodiazepinocarbazolone derivative 1 Patented [25]
Synonyms
PMID27841036-Compound-26
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MOA Inhibitor
Activity IC50 = 2.9 nM
External Link
 Compound Name Tetra-cyclic pyridophthalazinone derivative 1 Patented [25]
Synonyms
PMID27841036-Compound-25
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MOA Inhibitor
Activity IC50 = 5.1 nM
External Link
 Compound Name 3-phenyl isoquinolin-1(2H) derivative 1 Patented [25]
Synonyms
PMID27841036-Compound-20
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MOA Inhibitor
Activity IC50 < 10 nM
External Link
 Compound Name CPH-102 Preclinical [29]
Synonyms
IABP; INH2BP, Crimson Pharmaceutical; INH2BP, Octamer; PARP inhibitors, Crimson Pharmaceutical; PARP inhibitors, Octamer; CPH-101, Crimson Pharma
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MOA Inhibitor
External Link
 Compound Name PJ34 Preclinical [30]
Synonyms
344458-19-1; pj-34; N~2~,N~2~-DIMETHYL-N~1~-(6-OXO-5,6-DIHYDROPHENANTHRIDIN-2-YL)GLYCINAMIDE; CHEMBL372303; P34; 2-(dimethylamino)-N-(6-oxo-5,6-dihydrophenanthridin-2-yl)acetamide; Acetamide, N-(5,6-dihydro-6-oxo-2-phenanthridinyl)-2-(dimethylamino)-; UYJZZVDLGDDTCL-UHFFFAOYSA-N; PJ34(free base); 1xk9; SCHEMBL422317; ZINC8960; AC1L1J45; BDBM27497; CTK1B7701; MolPort-035-395-737; Ibrutinib (PCI32765 pound(c); HMS3651B06; BCP07990; HY-13688A; 2662AH; AKOS030229047; SB19292; DB08348; CS-1463; NCGC00370866-10; DA-42692; BC600341
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MOA Inhibitor
Activity IC50 = 10.9 nM
External Link
 Compound Name NU1025 Terminated [31]
MOA Inhibitor
Activity Ki = 48 nM
External Link
 Compound Name 3-Ethynylquinoline-8-carboxamide Investigative [32]
Synonyms
CHEMBL501330; 8-Quinolinecarboxamide, 3-ethynyl-; BDBM50255268
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MOA Inhibitor
Activity IC50 = 2300 nM
External Link
 Compound Name 2-(4-Amino-phenyl)-8-hydroxy-3H-quinazolin-4-one Investigative [33]
MOA Inhibitor
Activity IC50 = 289 nM
External Link
 Compound Name N-(4-Phenylthiazol-2-yl)isonicotinamide Investigative [34]
Synonyms
N-(4-phenyl-1,3-thiazol-2-yl)pyridine-4-carboxamide; CHEMBL482012; 5245-66-9; BAS 03572091; AC1Q5OBS; AC1LG7OX; CBMicro_015073; n-(4-phenyl-1,3-thiazol-2-yl)isonicotinamide; Cambridge id 5245669; Oprea1_303023; Oprea1_553111; SCHEMBL17107144; CTK4J5937; DTXSID30355050; MolPort-001-992-732; ZINC290573; STK483947; BDBM50255300; AKOS000569765; MCULE-9247268363; BIM-0015234.P001; N-(4-Phenyl-thiazol-2-yl)-isonicotinamide; ST50017829; N~4~-(4-phenyl-1,3-thiazol-2-yl)isonicotinamide; Z27772062
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MOA Inhibitor
Activity IC50 = 753 nM
External Link
 Compound Name 5-Chloro-2-methyl-3H-quinazolin-4-one Investigative [35]
MOA Inhibitor
Activity IC50 = 1200 nM
External Link
 Compound Name BZ3 Investigative [36]
Synonyms
5-METHOXYINDOLE; 1006-94-6; 5-Methoxy-1H-indole; 1H-Indole, 5-methoxy-; Femedol; 5-Methoxy indole; Indole, 5-methoxy-; Methoxy-5 indole; Indol-5-yl methyl ether; UNII-DQM3AS43PQ; Methoxy-5 indole [French]; 5-Methoxyindole, 99%; EINECS 213-745-3; DQM3AS43PQ; NSC 521752; CHEMBL280311; DWAQDRSOVMLGRQ-UHFFFAOYSA-N; MFCD00005674; 916979-77-6; 5Methoxyindole; 5-methoxyindol; 5-methoxy-indole; 3img; 3imc; PubChem7432; 1,3-dihydro-5-methyl-2H-Indol-2-one; ACMC-1BMAQ; 5-(methyloxy)-1H-indole; AC1Q4F1F; AC1L22NW; SCHEMBL74720; KSC177G3N; WLN: T
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MOA Inhibitor
External Link
 Compound Name 2-(3'-Methoxyphenyl) Benzimidazole-4-Carboxamide Investigative [31]
Synonyms
2-(3-methoxyphenyl)-1H-benzimidazole-4-carboxamide; CHEMBL134022; BZC; 1efy; AC1L1BMO; SCHEMBL4321727; CTK7A9229; NVVWVYYHTKCIAE-UHFFFAOYSA-N; ZINC11565446; BDBM50093373; DB04010; 2-(3'-Methoxyphenyl)-1-H-benzimidazole-4-carboxamide; 2-(3-methoxyphenyl)-1H-1,3-benzodiazole-4-carboxamide; 2-(3''-METHOXYPHENYL) BENZIMIDAZOLE-4-CARBOXAMIDE; 2-(3-Methoxy-phenyl)-1H-benzoimidazole-4-carboxylic acid amide
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MOA Inhibitor
Activity Ki = 6 nM
External Link
 Compound Name CEP-6800 Investigative [37]
Synonyms
UNII-0X7U7SRK9H; 0X7U7SRK9H; CHEMBL247374; 609848-02-4; SCHEMBL12256417; BDBM50197585; 1H-Cyclopenta(a)pyrrolo(3,4-C)carbazole-1,3(2H)-dione, 10-(aminomethyl)-4,5,6,7-tetrahydro-; 8-aminomethyl-1,2,3,11-tetrahydro-5,11-diaza-benzo[a]trindene-4,6-dione
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MOA Inhibitor
Activity IC50 = 18 nM
External Link
 Compound Name ANG-2864 Investigative [29]
Synonyms
PARP inhibitor (ischemia/cancer), Angion Biomedica
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MOA Inhibitor
External Link
 Compound Name 3-Methoxybenzamide Investigative [38]
Synonyms
5813-86-5; m-Methoxybenzamide; m-Anisamide; 3-Methoxy-benzamide; Benzamide, 3-methoxy-; UNII-M8502TLK98; EINECS 227-379-7; NSC 28589; NSC 209527; BRN 2206857; CHEMBL123978; VKPLPDIMEREJJF-UHFFFAOYSA-N; M8502TLK98; 3MB; 3pax; 5-methoxybenzamide; 3-methoxy-benzamid; ACMC-1ASRE; AC1Q5DMC; M-METHOXY BENZAMIDE; bmse000775; 3-Methoxybenzamide, 97%; Oprea1_695428; MLS001066418; 4-10-00-00326 (Beilstein Handbook Reference); cid_98487; SCHEMBL283787; AC1L407F; KS-00000VVU; CTK1H2082; VKPLPDIMEREJJF-UHFFFAOYSA-; DTXSID00206848
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MOA Inhibitor
Activity IC50 = 17000 nM
External Link
 Compound Name 2-Benzyl-2H-indazole-7-carboxamide Investigative [39]
Synonyms
CHEMBL1094951; SCHEMBL2268172
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MOA Inhibitor
Activity IC50 = 130 nM
External Link
 Compound Name 5-methylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione Investigative [40]
Synonyms
CHEMBL201723
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MOA Inhibitor
Activity IC50 = 5000 nM
External Link
 Compound Name 4-amino-1,8-naphthalimide Investigative [31]
Synonyms
1742-95-6; 4-Aminonaphthalimide; 6-AMINO-BENZO[DE]ISOQUINOLINE-1,3-DIONE; 6-Amino-1H-benzo[de]isoquinoline-1,3(2H)-dione; 4-Aminonaphthalene-1,8-dicarboximide; Naphthalimide, 4-amino-; DFP 1; 1H-Benz[de]isoquinoline-1,3(2H)-dione, 6-amino-; EINECS 217-110-1; BRN 0177185; 6-aminobenzo[de]isoquinoline-1,3-dione; PARP Inhibitor V, 4-ANI; CHEMBL338790; CHEBI:40071; SSMIFVHARFVINF-UHFFFAOYSA-N; 6-Amino-1H-benz(de)isoquinoline-1,3(2H)-dione; 4-AMINO-1,8 NAPHTHALIMIDE
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MOA Inhibitor
Activity IC50 = 26 nM
External Link
 Compound Name Pyrrolo[3,4-e]indole-1,3(2H,6H)-dione Investigative [40]
Synonyms
CHEMBL373066; pyrroloisoindoledione
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MOA Inhibitor
Activity IC50 = 750 nM
External Link
 Compound Name 8-Amino-6H,11H-indeno[1,2-c]isoquinolin-5-one Investigative [41]
Synonyms
SCHEMBL4662780; CHEMBL363363; BDBM27514; LQEYAIKMIJUZNT-UHFFFAOYSA-N; indeno[1,2-c]isoquinolinone, 2a; ZINC13652898; 5,6-Dihydro-5-oxo-8-amino-indeno[1,2-c]isoquinoline
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MOA Inhibitor
Activity IC50 = 300 nM
External Link
 Compound Name EB-47 Investigative [23]
Synonyms
EB 47; 366454-36-6; 5'-Deoxy-5'-[4-[2-[(2,3-dihydro-1-oxo-1H-isoindol-4-yl)amino]-2-oxoethyl]-1-piperazinyl]-5'-oxoadenosine Dihydrochloride; DTXSID40692822; ZINC98052573; NCGC00370771-01; KB-76747; FT-0667818; 4-[1-(6-Amino-9H-purin-9-yl)-1-deoxy-; A-D-ribofuranuronoyl]-N-(2,3-dihydro-1-oxo-1H-isoindol-4-yl)-1-piperazineacetamide Dihydrochloride; 2-{4-[(2R,3R,4S,5S)-5-(6-Amino-9H-purin-9-yl)-3,4-dihydroxyoxolane-2-carbonyl]piperazin-1-yl}-N-(1-oxo-2,3-dihydro-1H-isoindol-4-yl)acetamide (non-preferred name)
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MOA Inhibitor
External Link
 Compound Name BZ6 Investigative [36]
MOA Inhibitor
External Link
 Compound Name 2-(4-methoxyphenyl)quinoline-8-carboxamide Investigative [32]
Synonyms
CHEMBL481591; 655222-47-2; CTK1J6622; DTXSID70649086; BDBM50255383; AKOS030560276; 8-Quinolinecarboxamide, 2-(4-methoxyphenyl)-
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 1100 nM
External Link
 Compound Name 9-Amino-6H,11H-indeno[1,2-c]isoquinolin-5-one Investigative [41]
Synonyms
CHEMBL194155; SCHEMBL4078284; BDBM27515; BIBLEFNXUYTZIB-UHFFFAOYSA-N; indeno[1,2-c]isoquinolinone, 2b; ZINC13652899; 5,6-Dihydro-5-oxo-9-amino-indeno[1,2-c]isoquinoline
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MOA Inhibitor
Activity EC50 = 95 nM
External Link
 Compound Name (E)-N-(4-Phenylthiazol-2-yl) cinnamamide Investigative [34]
Synonyms
CHEMBL452100; 2-Cinnamamido-4-phenylthiazole; (2E)-3-phenyl-N-(4-phenyl-1,3-thiazol-2-yl)prop-2-enamide; 1107621-03-3; AC1LEPJR; ZINC60264; WOJRHCOBUKJCAJ-VAWYXSNFSA-N; MolPort-019-760-060; MolPort-001-931-977; HMS1397P15; STK173781; BDBM50255301; N-(4-phenylthiazol-2-yl)cinnamamide; AKOS000523355; MCULE-8934603681; BAS 00417267; ST4016450; 3-Phenyl-N-(4-phenyl-thiazol-2-yl)-acrylamide; AG-690/11629440; 3-phenyl-N-(4-phenyl-1,3-thiazol-2-yl)acrylamide; F0298-0058; A0793/0037152
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MOA Inhibitor
Activity IC50 = 224 nM
External Link
 Compound Name ANG-2684 Investigative [29]
Synonyms
ANG-3038; PARP-1 inhibitors (acute pancreatitis/stroke); PARP-1 inhibitors (acute pancreatitis/stroke), Angion Biomedica
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MOA Inhibitor
External Link
 Compound Name 4-methylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione Investigative [40]
Synonyms
CHEMBL380940; SCHEMBL5828673
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MOA Inhibitor
Activity IC50 = 2000 nM
External Link
 Compound Name 2,3-dihydro-1H-benzo[de]isoquinolin-1-one Investigative [42]
Synonyms
CHEMBL594596; 2,3-dihydro-benzo[de]isoquinolin-1-one; SCHEMBL832168; ZINC24216; BDBM50306285; FCH1866210
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MOA Inhibitor
Activity IC50 = 540 nM
External Link
 Compound Name 5-amino-3,4-dihydroisoquinolin-1(2H)-one Investigative [42]
Synonyms
129075-53-2; CHEMBL594759; SCHEMBL7581623; RTPKPVYTPRJRBY-UHFFFAOYSA-N; ZINC45353622; BDBM50306284; AKOS023598631; AB53700; FCH1123505; KS-9128; CM10348; AJ-110485; 5-amino-3,4-dihydro-1(2H)-isoquinolinone; EN300-254419
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MOA Inhibitor
Activity IC50 = 410 nM
External Link
 Compound Name KR-33889 Investigative [29]
Synonyms
KR-34285; PARP-1 inhibitors (myocardial infarction), KRICT
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MOA Inhibitor
External Link
 Compound Name 4-(5-Morpholin-4-yl-pentyl)-2H-phthalazin-1-one Investigative [43]
Synonyms
CHEMBL194684
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MOA Inhibitor
Activity IC50 = 119 nM
External Link
 Compound Name AG-014376 Investigative [44]
Synonyms
CHEMBL361489; SCHEMBL7159231; BDBM50154730; 6-(4-Dimethylaminomethyl-phenyl)-3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-one
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 6.4 nM
External Link
 Compound Name 3-Hydroxy-benzamide Investigative [33]
Synonyms
3-hydroxybenzamide; 618-49-5; benzamide, 3-hydroxy-; CHEMBL419424; 3-Hydroxy benzamide; NSC379289; 3-hydroxybenzenecarboxamide; AC1Q4ZB3; AC1L7W2U; ACMC-1B71B; Oprea1_435073; SCHEMBL161861; 3-Hydroxybenzamide, AldrichCPR; CTK2F7291; DTXSID90321635; NGMMGKYJUWYIIG-UHFFFAOYSA-N; MolPort-001-791-593; ZINC1590754; KM0548; BDBM50068769; 9282AB; ANW-33964; 3-HYDROXY-BENZOIC ACID,AMIDE; SBB079277; AKOS000207073; VZ26952; NSC-379289; MB00281; MCULE-9599926365; NCGC00323509-01; KB-32185; CJ-25437; AJ-27681; CJ-05592; SC-47787
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 9100 nM
External Link
 Compound Name 8-Methoxy-2-phenyl-3H-quinazolin-4-one Investigative [33]
MOA Inhibitor
Activity IC50 > 10000 nM
External Link
 Compound Name Quinoline-8-carboxamide Investigative [32]
Synonyms
8-Quinolinecarboxamide; 55706-61-1; CCRIS 6967; CHEMBL502330; HPQRQAOVNXWEEQ-UHFFFAOYSA-N; 8-Carbamoylquinoline; 8-Quinolinecarboxamide #; AC1L44SC; SCHEMBL460456; CTK5A4047; quinoline-8-carboxylic acid amide; DTXSID00204243; MolPort-005-722-305; ZINC6095019; BDBM50255266; AKOS008969900; NE38855; MCULE-7978956907; LS-188644; KB-259682
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MOA Inhibitor
Activity IC50 = 1900 nM
External Link
 Compound Name 9-Fluoro-6H,11H-indeno[1,2-c]isoquinolin-5-one Investigative [41]
Synonyms
CHEMBL190895; BDBM27513; indeno[1,2-c]isoquinolinone, 1e; 9-Fluoro-5,6-dihydro-11H-indeno[1,2-c]isoquinoline-5-one
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 180 nM
External Link
 Compound Name 8-Methyl-2-(4-nitro-phenyl)-3H-quinazolin-4-one Investigative [33]
MOA Inhibitor
Activity IC50 = 104 nM
External Link
 Compound Name 2H-Isoquinolin-1-one Investigative [33]
Synonyms
1-Hydroxyisoquinoline; 491-30-5; Isoquinolin-1(2H)-one; isoquinolin-1-ol; 1-Isoquinolinol; Isocarbostyril; 1(2H)-ISOQUINOLINONE; Isoquinolin-1-one; 489453-23-8; 1(2H)-Isoquinolone; 1,2-dihydroisoquinolin-1-one; 1-hydroxyisoquinolin; isoquinolinol; 87602-67-3; 1(2H)-ISOQUINILONE; Isocarbostyril, 98%; UNII-95EG3HGG1P; 95EG3HGG1P; Isoquinolinone; CHEMBL339695; CHEBI:18350; VDBNYAPERZTOOF-UHFFFAOYSA-N; 1-isoquinolone; oxidoisoquinolinium; EINECS 207-732-1; Isocarbostyril(1-hydroxyisoquinoline); NSC 27273
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MOA Inhibitor
Activity IC50 = 9 nM
External Link
 Compound Name KU-58684 Investigative [34]
Synonyms
SCHEMBL863338; 623578-11-0
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MOA Inhibitor
External Link
 Compound Name 2,8-Dimethyl-3H-quinazolin-4-one Investigative [33]
MOA Inhibitor
Activity IC50 = 490 nM
External Link
 Compound Name 5-aminoisoquinolin-1(2H)-one Investigative [32]
Synonyms
93117-08-9; 5-amino-2H-isoquinolin-1-one; 5-AMINOISOQUINOLIN-1-OL; 5-amino-1,2-dihydroisoquinolin-1-one; 5-AIQ; CHEMBL446240; 5-Amino-2H-isoquinoin-1-one; 5-AMINO-1(2H)-ISOQUINOLINONE; 5-aminoisoquinolinone; 4pnq; 32X; AC1Q6DVG; AC1L1CUR; 5-Amino-1-isoquinolinol; SCHEMBL215327; 5-Amino-1-hydroxyisoquinoline; BDBM27503; 5-amino-isoquinolin-1(2h)-one; 5-amino isoquinolin-1(2h)-one; CTK5H2122; DTXSID90274354; 1(2H)-Isoquinolinone,5-amino-; MolPort-008-423-043; MolPort-004-803-197
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MOA Inhibitor
Activity IC50 = 940 nM
External Link
 Compound Name INO-1002 Investigative [29]
Synonyms
PARP inhibitors, Inotek; PARP inhibitor (erectile dysfunction), Inotek; PARP inhibitor (prostate nerve damage), Inotek; Poly (ADP ribose) polymerase inhibitor (erectile dysfunction), Inotek; Poly (ADP ribose) polymerase inhibitor (prostate nerve damage), Inotek
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MOA Inhibitor
External Link
 Compound Name 3-(4-aminophenyl)quinoxaline-5-carboxamide Investigative [34]
Synonyms
CHEMBL443077; quinoxaline analogue, 3f; SCHEMBL7112515
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MOA Inhibitor
Activity IC50 = 87 nM
External Link
 Compound Name 2-phenylpyrazolo-[1,5-a]pyridine-7-carboxamide Investigative [39]
Synonyms
2-phenylpyrazolo[1,5-a]pyridine-7-carboxamide; 1196713-16-2; ZINC64337832; DA-47424
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MOA Inhibitor
External Link
 Compound Name 4-benzylphthalazin-1(2H)-one Investigative [34]
Synonyms
4-Benzyl-1(2H)-phthalazinone; 32003-14-8; 4-Benzyl-2H-phthalazin-1-one; 4-benzyl-1,2-dihydrophthalazin-1-one; CHEMBL66761; JUCCMEHWBGPJKS-UHFFFAOYSA-N; benzylphthalazinone; phthalazinone, 1; 4-benzyl-phthalazone; AC1LDDNC; SMR000135223; AC1Q6GZZ; ChemDiv2_000142; Cambridge id 5241846; Oprea1_151142; Oprea1_623913; CBDivE_015258; MLS000530246; SCHEMBL863462; CTK4G8063; BDBM27660; DTXSID30346948; MolPort-001-796-654; HMS2379K10; HMS1369G10; 4-benzyl-2-hydrophthalazin-1-one; 4-Benzyl-1(2H)-phthalazinone #
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MOA Inhibitor
Activity IC50 = 770 nM
External Link
 Compound Name 3-Methylquinoline-8-carboxamide Investigative [32]
Synonyms
CHEMBL504998; 8-Quinolinecarboxamide, 3-methyl-; BDBM50255267
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MOA Inhibitor
Activity IC50 = 3400 nM
External Link
 Compound Name 2-(4-Chlorophenyl)-5-Quinoxalinecarboxamide Investigative [38]
Synonyms
3-(4-CHLOROPHENYL)QUINOXALINE-5-CARBOXAMIDE; 4tju; 1wok; AC1LCVX7; quinoxaline analogue, 3b; SCHEMBL424209; 3-(4-chloro-phenyl)-quinoxaline-5-carboxylic acid amide; CTK8F4675; BDBM27720; ZINC1489510; DB03509; 489457-67-2
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MOA Inhibitor
External Link
 Compound Name 2-(4-Methoxy-phenyl)-8-methyl-3H-quinazolin-4-one Investigative [33]
MOA Inhibitor
Activity IC50 = 891 nM
External Link
 Compound Name HYDAMTIQ Investigative [29]
Synonyms
PARP-1 inhibitor (brain ischemia), University of Perugia
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MOA Inhibitor
External Link
 Compound Name 8-Nitro-6H,11H-indeno[1,2-c]isoquinolin-5-one Investigative [41]
Synonyms
SCHEMBL4661629; CHEMBL370673; BDBM27510; SWBDUXDIPMGDNO-UHFFFAOYSA-N; indeno[1,2-c]isoquinolinone, 1b; ZINC13652894; 5,6-dihydro-5-oxo-8-nitro-indeno[1,2-c]isoquinoline; 8-Nitro-5,6-dihydro-11H-indeno[1,2-c]isoquinoline-5-one
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MOA Inhibitor
Activity IC50 = 500 nM
External Link
 Compound Name PD-128763 Investigative [38]
Synonyms
5-Methyl-3,4-dihydroisoquinolin-1(2H)-one; 129075-56-5; 3,4-Dihydro-5-methyl-1(2H)-isoquinolinone; 3,4-DIHYDRO-5-METHYL-ISOQUINOLINONE; 1(2H)-Isoquinolinone, 3,4-dihydro-5-methyl-; CHEBI:41928; PD128763; CHEMBL125200; 5-methyl-3,4-dihydro-2H-isoquinolin-1-one; 3,4-dihydro-5-methylisoquinolinone; 1(2H)-Isoquinolinone,3,4-dihydro-5-methyl-; 5-methyl-1,2,3,4-tetrahydroisoquinolin-1-one; DHQ; PD 128763; dihydroisoquinolinone, 1; AC1L3WIO; ACMC-1C7L4; SCHEMBL831538; AMBZ0075; KS-00000QFP; CTK4B6146; BDBM27682
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 70 nM
External Link
 Compound Name 8-Methyl-2-phenyl-3H-quinazolin-4-one Investigative [33]
MOA Inhibitor
Activity IC50 = 795 nM
External Link
 Compound Name TI3 Investigative [36]
Synonyms
RB106; CHEMBL419499; [(2S)-2-SULFANYL-3-PHENYLPROPANOYL]-GLY-(5-PHENYLPROLINE); 1qf2; AC1L9LL2; BDBM50051785; DB02669; N-[(S)-2-Mercapto-3-phenylpropionyl]-Gly-[(5R)-5-phenyl-L-Pro-]-OH; N-[(2S)-3-phenyl-2-sulfanylpropanoyl]glycyl-(5R)-5-phenyl-L-proline; (2S,5R)-5-phenyl-1-[2-[[(2S)-3-phenyl-2-sulfanylpropanoyl]amino]acetyl]pyrrolidine-2-carboxylic acid; (2S,5R)-1-[2-((S)-2-Mercapto-3-phenyl-propionylamino)-acetyl]-5-phenyl-pyrrolidine-2-carboxylic acid
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 3-aminobenzo[c][1,5]naphthyridin-6(5H)-one Investigative [34]
Synonyms
CHEMBL106154; Benzo[c]-1,5-naphthyridin-6(5H)-one, 3-amino-; SCHEMBL12750402; BDBM50130580; 433726-73-9
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 180 nM
External Link
 Compound Name S-111 Investigative [29]
Synonyms
PARP1 inhibitor (cancer), Sentinel Oncology
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name Thieno-phenanthridin-6-one Investigative [23]
MOA Inhibitor
External Link
 Compound Name 3-Morpholin-4-ylmethyl-5H-phenanthridin-6-one Investigative [43]
Synonyms
CHEMBL194535
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 23 nM
External Link
 Compound Name 1,2,3,4,4a,5-hexahydrophenanthridin-6(10bH)-one Investigative [34]
Synonyms
CHEMBL84044; 7403-93-2; NSC403412; AC1L83AN; SCHEMBL6645911; DTXSID70323238; BDBM50131013; NSC-403412; 2,3,4,4a,5,10b-hexahydro-1H-phenanthridin-6-one; 1,3,4,4a,5,10b-Hexahydro-2H-phenanthridin-6-one
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 7500 nM
External Link
 Compound Name 8-Hydroxy-2-(4-nitro-phenyl)-3H-quinazolin-4-one Investigative [33]
MOA Inhibitor
Activity IC50 = 105 nM
External Link
 Compound Name 2-(4-Amino-phenyl)-8-methyl-3H-quinazolin-4-one Investigative [33]
MOA Inhibitor
Activity IC50 = 504 nM
External Link
 Compound Name 4-(4-Morpholin-4-yl-butyl)-2H-phthalazin-1-one Investigative [43]
Synonyms
CHEMBL373210
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MOA Inhibitor
Activity IC50 = 950 nM
External Link
 Compound Name 2-phenyl-2H-benzo[d][1,2,3]triazole-4-carboxamide Investigative [39]
Synonyms
CHEMBL1096560; SCHEMBL2265205
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 71 nM
External Link
 Compound Name 2-phenyl-2H-indazole-7-carboxamide Investigative [39]
Synonyms
CHEMBL594298; SCHEMBL1422404; BDBM50306166
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 24 nM
External Link
 Compound Name Carba-Nicotinamide-Adenine-Dinucleotide Investigative [38]
Synonyms
Carba-NAD; Carbanicotinamide adenine dinucleotide; 112345-60-5; AC1L4TS7; AC1Q5J0L; SCHEMBL16445201; 5'-o-{[({[(1r,2r,3s,4r)-4-(3-carbamoylpyridinium-1-yl)-2,3-dihydroxycyclopentyl]methoxy}phosphinato)oxy](hydroxy)phosphoryl}adenosine; [[(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] [(1R,2R,3S,4R)-4-(3-carbamoylpyridin-1-ium-1-yl)-2,3-dihydroxycyclopentyl]methyl phosphate; Adenosine 5'-(trihydrogen diphosphate), 5'-((4-(3-(aminocarbonyl)pyridinio)-2,3-dihydroxycyclopentyl)m
    Click to Show/Hide
MOA Inhibitor
External Link
 Compound Name 3-aminobenzamide Investigative [30]
Synonyms
3544-24-9; m-Aminobenzamide; Benzamide, 3-amino-; 3-Amino-benzamide; Benzamide, m-amino-; meta-aminobenzamide; 3-ABA; 3-Aminobenzimide; 3-amino benzamide; aniline-3-carboxamide; 3-aminobenzoic acid amide; UNII-8J365YF1YH; CCRIS 3925; EINECS 222-586-9; NSC 36962; BRN 2802373; PARP Inhibitor I, 3-ABA; 3-H2NC6H4CONH2; CHEMBL81977; 3-AB; 8J365YF1YH; CHEBI:64042; GSCPDZHWVNUUFI-UHFFFAOYSA-N; MFCD00007989; 3-Aminobenzamide, 98%; SR-01000075657; HSDB 7581; 3-azanylbenzamide; m-amino benzamide; 4pml; 3-Aminobenzaminde
    Click to Show/Hide
MOA Inhibitor
Activity Ki = 3100 nM
External Link
 Compound Name 3-Ethenylquinoline-8-carboxamide Investigative [32]
Synonyms
CHEMBL481793; 8-Quinolinecarboxamide, 3-ethenyl-; BDBM50255270
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MOA Inhibitor
Activity IC50 = 5800 nM
External Link
 Compound Name 3-Phenylquinoline-8-carboxamide Investigative [32]
Synonyms
CHEMBL450259; BDBM50255264
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MOA Inhibitor
Activity IC50 = 15000 nM
External Link
 Compound Name 3-(4-methoxyphenyl)quinoxaline-5-carboxamide Investigative [34]
Synonyms
CHEMBL519443; quinoxaline analogue, 3e; SCHEMBL7045177
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 71 nM
External Link
 Compound Name TI4 Investigative [36]
MOA Inhibitor
External Link
 Compound Name Benzo[c][1,5]naphthyridin-6(5H)-one Investigative [34]
Synonyms
CHEMBL320031; Benzo[c]-1,5-naphthyridin-6(5H)-one; SCHEMBL12750384; BDBM50130585; 5H-Benzo[c][1,5]naphthyridin-6-one; Benzo[c][1,5]naphthyridine-6(5H)-one
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 116 nM
External Link
 Compound Name 3-(4-cyanophenyl)quinoxaline-5-carboxamide Investigative [34]
Synonyms
CHEMBL481603; quinoxaline analogue, 3c; SCHEMBL7108289
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MOA Inhibitor
Activity IC50 = 101 nM
External Link
 Compound Name 1,7,8,9-tetrahydro-1,5-diaza-trindene-4,6-dione Investigative [40]
Synonyms
CHEMBL201907; SCHEMBL2086780; ZINC28569089
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MOA Inhibitor
Activity IC50 = 40 nM
External Link
 Compound Name 8-Fluoro-6H,11H-indeno[1,2-c]isoquinolin-5-one Investigative [41]
Synonyms
CHEMBL370045; BDBM27512; indeno[1,2-c]isoquinolinone, 1d; ZINC13652896; 8-Fluoro-5,6-dihydro-11H-indeno[1,2-c]isoquinoline-5-one
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 225 nM
External Link
 Compound Name 8-Hydroxy-2-phenyl-3H-quinazolin-4-one Investigative [33]
MOA Inhibitor
Activity IC50 = 1034 nM
External Link
 Compound Name 8-Methoxy-2-(4-nitro-phenyl)-3H-quinazolin-4-one Investigative [33]
MOA Inhibitor
Activity IC50 > 10000 nM
External Link
 Compound Name 2-(4-Chlorophenyl)-2H-indazole-7-carboxamide Investigative [39]
Synonyms
CHEMBL1099295; SCHEMBL2264064
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MOA Inhibitor
Activity IC50 = 24 nM
External Link
 Compound Name BPI-704001 Investigative [29]
Synonyms
BPI-705001; BPI-715001; PARP-1 inhibitors (cancer); PARP-1 inhibitors (cancer), Beta Pharma
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MOA Inhibitor
External Link
 Compound Name Pyrrolo[3,4-c]carbazole-1,3(2H,6H)-dione Investigative [40]
Synonyms
CHEMBL370869; SCHEMBL5381581
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MOA Inhibitor
Activity IC50 = 10000 nM
External Link
 Compound Name 2-Methylquinoline-8-carboxamide Investigative [32]
Synonyms
CHEMBL471966; 8-Quinolinecarboxamide, 2-methyl-; SCHEMBL422282; BDBM50255329; AKOS022882220
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 500 nM
External Link
 Compound Name 8-Methoxy-2-methyl-3H-quinazolin-4-one Investigative [33]
MOA Inhibitor
External Link
 Compound Name 3-Prop-1-ynylquinoline-8-carboxamide Investigative [32]
Synonyms
CHEMBL504903; ZINC40829471
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 2200 nM
External Link
 Compound Name 2-(2-Chlorophenyl)-2H-indazole-7-carboxamide Investigative [39]
Synonyms
CHEMBL1094952; SCHEMBL2265265
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MOA Inhibitor
Activity IC50 = 100 nM
External Link
 Compound Name 2-(3-Piperidin-1-yl-propyl)-3H-quinazolin-4-one Investigative [35]
MOA Inhibitor
Activity IC50 = 1100 nM
External Link
 Compound Name 3-Ethylquinoline-8-carboxamide Investigative [32]
Synonyms
CHEMBL453989; 8-Quinolinecarboxamide, 3-ethyl-; BDBM50255269
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MOA Inhibitor
Activity IC50 = 3700 nM
External Link
 Compound Name A-620223 Investigative [29]
Synonyms
A-866111; A-966492; ABT-472; ABT-999; PARP inhibitor, Abbott; PARP inhibitors, Abbott; Poly (ADP)ribose polymer inhibitor, Abbott; Poly (ADP)ribose inhibitors (cancer), Abbott
    Click to Show/Hide
MOA Inhibitor
Activity EC50 = 3 nM
External Link
 Compound Name DR2313 Investigative [23]
MOA Inhibitor
External Link
 Compound Name 2-(4-Azido-phenyl)-8-methoxy-3H-quinazolin-4-one Investigative [33]
MOA Inhibitor
External Link
 Compound Name 2-(3-Chlorophenyl)-2H-indazole-7-carboxamide Investigative [39]
Synonyms
CHEMBL1094953; SCHEMBL2265628
    Click to Show/Hide
MOA Inhibitor
Activity IC50 = 14 nM
External Link
 Compound Name 2-(4-Hydroxy-phenyl)-8-methyl-3H-quinazolin-4-one Investigative [33]
MOA Inhibitor
Activity IC50 = 1200 nM
External Link
 Compound Name 2-ethylquinoline-8-carboxamide Investigative [32]
Synonyms
CHEMBL526128; 8-Quinolinecarboxamide, 2-ethyl-; BDBM50255330
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MOA Inhibitor
Activity IC50 = 800 nM
External Link
 Compound Name 2-phenylquinoline-8-carboxamide Investigative [32]
Synonyms
CHEMBL480429; SCHEMBL6442515; ZINC3939668
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MOA Inhibitor
Activity IC50 = 900 nM
External Link
 Compound Name BZ5 Investigative [36]
MOA Inhibitor
External Link
 Compound Name ME0328 Investigative [45]
Synonyms
ME-0328; compound 5b [PMID 24188023]
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MOA Inhibitor
Activity IC50 = 6300 nM
External Link
 Compound Name [2(R,S)-2-Sulfanylheptanoyl]-Phe-Ala Investigative [36]
Synonyms
TI1; AC1NRDCJ; 1qf1; DB02597; N-[(2S)-2-sulfanylheptanoyl]-L-phenylalanyl-L-alanine; N-[N-[(S)-2-Mercaptoheptanoyl]-L-phenylalanyl]-L-alanine; (2S)-2-[[(2S)-3-phenyl-2-[[(2S)-2-sulfanylheptanoyl]amino]propanoyl]amino]propanoic acid; (2S)-2-[(2S)-3-phenyl-2-[(2S)-2-sulfanylheptanamido]propanamido]propanoic
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MOA Inhibitor
External Link
 Compound Name S-070 Investigative [29]
Synonyms
S-158; Targeted synergy program (solid tumor), Sentinel Oncology; Chk1/PARP-1 inhibitors (cancer); Chk1/PARP-1 inhibitors (cancer), Sentinel Oncology
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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 [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
 Compound Name Atezolizumab Approved [5]
External Link
 Compound Name Bavencio Approved [5]
External Link
 Compound Name Tebentafusp Approved [47]
External Link
 Compound Name 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
    Click to Show/Hide
External Link
 Compound Name 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))-
    Click to Show/Hide
External Link
 Compound Name Ramucirumab Approved [50]
Synonyms
LY3009806
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External Link
 Compound Name 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
 Compound Name Antacids Approved [52]
External Link
 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 [53]
Synonyms
Carbamazepine (iv, epilepsy); Carbamazepine (iv, epilepsy), Lundbeck; Carbamazepine (iv, epilepsy), Ovation Pharmaceuticals
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External Link
 Compound Name Margetuximab Approved [5]
External Link
 Compound Name Nivolumab Approved [5]
External Link
 Compound Name 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)-
    Click to Show/Hide
External Link
 Compound Name Zolbetuximab Phase 3 [55]
Synonyms
IMAB362
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External Link
 Compound Name Tusamitamab ravtansine Phase 3 [56]
Synonyms
SAR408701
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External Link
 Compound Name Andecaliximab Phase 3 [57]
External Link
 Compound Name ABP 980 Phase 3 [58]
External Link
 Compound Name GS-5745 Phase 3 [49]
External Link
 Compound Name 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)
    Click to Show/Hide
External Link
 Compound Name Lonsurf Phase 3 [5]
External Link
 Compound Name GDC-0068 Phase 3 [49]
Synonyms
RG7440
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External Link
 Compound Name 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
    Click to Show/Hide
External Link
 Compound Name RG3638 Phase 3 [61]
Synonyms
Onartuzumab
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External Link
 Compound Name G17DT Phase 3 [62]
Synonyms
Gastrimmune; Insegia
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External Link
 Compound Name DE-766 Phase 3 [63]
External Link
 Compound Name 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
    Click to Show/Hide
External Link
 Compound Name Nelipepimut S Phase 3 [65]
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)-
    Click to Show/Hide
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 [66]
Synonyms
CNS modulator (spasticity), Osmotica
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External Link
 Compound Name Oraxol Phase 3 [5]
External Link
 Compound Name 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
 Compound Name Evorpacept Phase 2/3 [67]
Synonyms
ALX148
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 Compound Name BNT141 Phase 2 [68]
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 Compound Name Anti-LAG3 Phase 2 [58]
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 Compound Name GSK1292263 Phase 2 [69]
External Link
 Compound Name MM-111 Phase 2 [70]
External Link
 Compound Name 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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External Link
 Compound Name 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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External Link
 Compound Name 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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External Link
 Compound Name 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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External Link
 Compound Name BAY-57-9352 Phase 2 [49]
Synonyms
Telatinib; Bay 57-9352
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External Link
 Compound Name Bemarituzumab Phase 2 [74]
External Link
 Compound Name PEGPH20 Phase 2 [5]
External Link
 Compound Name Plevitrexed (R)-isomer Phase 2 [75]
Synonyms
YW3548
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External Link
 Compound Name APR-246 Phase 2 [76]
Synonyms
Eprenetapopt
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 Compound Name CRS-207 Phase 2 [65]
External Link
 Compound Name Opdivo + Yervoy Phase 3 [5]
External Link
 Compound Name CT-041 Phase 1/2 [77]
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 Compound Name BPX-601 Phase 1/2 [78]
External Link
 Compound Name Anti-MUC1 CAR-T cells Phase 1/2 [79]
External Link
 Compound Name Anti-Mesothelin CAR-T cells Phase 1/2 [80]
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 Compound Name Anti-HER2 CAR-T Phase 1/2 [81]
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 Compound Name CAR-T Cells targeting EpCAM Phase 1/2 [82]
External Link
 Compound Name 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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 Compound Name ASP2138 Phase 1 [84]
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 Compound Name SAR443216 Phase 1 [85]
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 Compound Name AMG 199 Phase 1 [86]
External Link
 Compound Name AMG 910 Phase 1 [87]
External Link
 Compound Name 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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External Link
 Compound Name HER2-specific CAR T cell Phase 1 [89]
External Link
 Compound Name Anti-CEA-CAR T Phase 1 [90]
External Link
 Compound Name XR-5944 Phase 1 [91]
Synonyms
MLN-944; XR-11576 analogs; XR-5000 analogs; XR-5942
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External Link
 Compound Name A168 Phase 1 [92]
External Link
 Compound Name EGFR806-specific CAR T cell Phase 1 [93]
External Link
 Compound Name AbGn-107 Phase 1 [5]
External Link
 Compound Name FPA144 Phase 1 [58]
External Link
 Compound Name Minnelide 001 Phase 1 [49]
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 Compound Name CAR-T cells targeting EpCAM Phase 1 [94]
External Link
 Compound Name Anti-CEA CAR-T cells Phase 1 [95]
External Link
 Compound Name EPCAM-targeted CAR-T cells Clinical trial [96]
External Link
 Compound Name PMID28460551-Compound-1 Patented [97]
External Link
 Compound Name Conjugated 3-(indolyl)-and 3-(azaindolyl)-4-arylmaleimide compound 1 Patented [98]
Synonyms
PMID28621580-Compound-WO2012084683c62
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External Link
 Compound Name TOPIXANTRONE HYDROCHLORIDE Discontinued in Phase 2 [99]
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 [100]
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 [101]
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 [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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External Link
 Compound Name Kanjinti Application submitted [5]
External Link
 Compound Name Anti-CD9 mab Investigative [103]
Synonyms
ALB-6; Anti-CD9 mAb (gastric cancer); Anti-CD9 mAb (gastric cancer), Osaka University
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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 oxaliplatin resistance of gastric cancer CD133+?stem cells by promoting PARP1 mRNA stability. Cell Mol Life Sci. 2022 Feb 18;79(3):135. doi: 10.1007/s00018-022-04129-0.
Ref 3 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
Ref 4 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 5 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 6 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 7 ClinicalTrials.gov (NCT04104776) A Study of CPI-0209 in Patients With Advanced Tumors. U.S. National Institutes of Health.
Ref 8 National Cancer Institute Drug Dictionary (drug id 756211).
Ref 9 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 10 Clinical pipeline report, company report or official report of HaiHe Biopharma.
Ref 11 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 12 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.
Ref 13 A selective inhibitor of EZH2 blocks H3K27 methylation and kills mutant lymphoma cells. Nat Chem Biol. 2012 Nov;8(11):890-6. doi: 10.1038/nchembio.1084. Epub 2012 Sep 30.
Ref 14 Selective inhibition of Ezh2 by a small molecule inhibitor blocks tumor cells proliferation. Proc Natl Acad Sci U S A. 2012 Dec 26;109(52):21360-5. doi: 10.1073/pnas.1210371110. Epub 2012 Dec 10.
Ref 15 An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34. doi: 10.1021/cb400133j. Epub 2013 Apr 24.
Ref 16 Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett. 2012 Oct 19;3(12):1091-6. doi: 10.1021/ml3003346. eCollection 2012 Dec 13.
Ref 17 TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751.
Ref 18 beta-1,2,3-Triazolyl-nucleosides as nicotinamide riboside mimics. Nucleosides Nucleotides Nucleic Acids. 2009 Mar;28(3):238-59. doi: 10.1080/15257770902865415.
Ref 19 Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase-3. J Med Chem. 2009 May 14;52(9):3108-11. doi: 10.1021/jm900052j.
Ref 20 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 21 Inhibition of poly (ADP-ribose) polymerase as a protective effect of nicaraven in ionizing radiation- and ara-C-induced cell death. Anticancer Res. 2006 Sep-Oct;26(5A):3421-7.
Ref 22 Tricyclic benzimidazoles as potent poly(ADP-ribose) polymerase-1 inhibitors. J Med Chem. 2003 Jan 16;46(2):210-3. doi: 10.1021/jm0255769.
Ref 23 Poly(ADP-ribose) polymerase and the therapeutic effects of its inhibitors. Nat Rev Drug Discov. 2005 May;4(5):421-40. doi: 10.1038/nrd1718.
Ref 24 Preclinical Characterization of AZD5305, A Next-Generation, Highly Selective PARP1 Inhibitor and Trapper. Clin Cancer Res. 2022 Nov 1;28(21):4724-4736.
Ref 25 PARP inhibitors as antitumor agents: a patent update (2013-2015). Expert Opin Ther Pat. 2017 Mar;27(3):363-382. doi: 10.1080/13543776.2017.1259413. Epub 2016 Nov 21.
Ref 26 Clinical pipeline report, company report or official report of Allarity Therapeutics.
Ref 27 AMXI-5001, a novel dual parp1/2 and microtubule polymerization inhibitor for the treatment of human cancers. Am J Cancer Res. 2020 Aug 1;10(8):2649-2676. eCollection 2020.
Ref 28 NMS-P293, a PARP-1 selective inhibitor with no trapping activity and high CNS penetration, possesses potent in vivo efficacy and represents a novel therapeutic option for brain localized metastases and glioblastoma. Cancer Res 2018;78(13 Suppl):Abstract nr 4843.
Ref 29 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2771).
Ref 30 Diabetic endothelial dysfunction: the role of poly(ADP-ribose) polymerase activation. Nat Med. 2001 Jan;7(1):108-13. doi: 10.1038/83241.
Ref 31 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. doi: 10.1093/nar/28.1.235.
Ref 32 Design, synthesis, and evaluation in vitro of quinoline-8-carboxamides, a new class of poly(adenosine-diphosphate-ribose)polymerase-1 (PARP-1) inhibitor. J Med Chem. 2009 Feb 12;52(3):868-77. doi: 10.1021/jm8013629.
Ref 33 Resistance-modifying agents. 5. Synthesis and biological properties of quinazolinone inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase (PARP). J Med Chem. 1998 Dec 17;41(26):5247-56. doi: 10.1021/jm980273t.
Ref 34 Design, synthesis, and cytoprotective effect of 2-aminothiazole analogues as potent poly(ADP-ribose) polymerase-1 inhibitors. J Med Chem. 2009 Feb 12;52(3):718-25. doi: 10.1021/jm800902t.
Ref 35 Rational approaches to discovery of orally active and brain-penetrable quinazolinone inhibitors of poly(ADP-ribose)polymerase. J Med Chem. 2004 Aug 12;47(17):4151-4. doi: 10.1021/jm0499256.
Ref 36 Identification of potent nontoxic poly(ADP-Ribose) polymerase-1 inhibitors: chemopotentiation and pharmacological studies. Clin Cancer Res. 2003 Jul;9(7):2711-8.
Ref 37 Novel poly(ADP-ribose) polymerase-1 inhibitors. Bioorg Med Chem Lett. 2007 Jan 15;17(2):542-5. doi: 10.1016/j.bmcl.2006.10.010. Epub 2006 Oct 10.
Ref 38 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
Ref 39 Discovery of 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide (MK-4827): a novel oral poly(ADP-ribose)polymerase (PARP) inhibitor efficacious in BRCA-1 and -2 mutant tumors. J Med Chem. 2009 Nov 26;52(22):7170-85. doi: 10.1021/jm901188v.
Ref 40 Synthesis and structure-activity relationships of novel poly(ADP-ribose) polymerase-1 inhibitors. Bioorg Med Chem Lett. 2006 Feb 15;16(4):938-42. doi: 10.1016/j.bmcl.2005.10.099. Epub 2005 Nov 15.
Ref 41 Discovery of potent poly(ADP-ribose) polymerase-1 inhibitors from the modification of indeno[1,2-c]isoquinolinone. J Med Chem. 2005 Aug 11;48(16):5100-3. doi: 10.1021/jm0502891.
Ref 42 Discovery and SAR of novel, potent and selective hexahydrobenzonaphthyridinone inhibitors of poly(ADP-ribose)polymerase-1 (PARP-1). Bioorg Med Chem Lett. 2010 Jan 15;20(2):448-52. doi: 10.1016/j.bmcl.2009.12.002. Epub 2009 Dec 4.
Ref 43 4-Phenyl-1,2,3,6-tetrahydropyridine, an excellent fragment to improve the potency of PARP-1 inhibitors. Bioorg Med Chem Lett. 2005 Oct 1;15(19):4221-5. doi: 10.1016/j.bmcl.2005.06.094.
Ref 44 Design, synthesis, and evaluation of 3,4-dihydro-2H-[1,4]diazepino[6,7,1-hi]indol-1-ones as inhibitors of poly(ADP-ribose) polymerase. J Med Chem. 2004 Oct 21;47(22):5467-81. doi: 10.1021/jm030513r.
Ref 45 Chemical probes to study ADP-ribosylation: synthesis and biochemical evaluation of inhibitors of the human ADP-ribosyltransferase ARTD3/PARP3. J Med Chem. 2013 Dec 12;56(23):9556-68. doi: 10.1021/jm401394u. Epub 2013 Nov 22.
Ref 46 FDA Approved Drug Products from FDA Official Website. 2023. Application Number: 217759.
Ref 47 FDA Approved Drug Products from FDA Official Website. 2022. Application Number: 761228.
Ref 48 FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 022059.
Ref 49 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 50 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7390).
Ref 51 ClinicalTrials.gov (NCT04499924) Tucatinib, Trastuzumab, Ramucirumab, and Paclitaxel Versus Paclitaxel and Ramucirumab in Previously Treated HER2+ Gastroesophageal Cancer (MOUNTAINEER-02). U.S. National Institutes of Health.
Ref 52 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 53 ClinicalTrials.gov (NCT01128959) Study to Assess the Safety and Tolerability of Intravenous Carbamazepine in Adults With Epilepsy. U.S. National Institutes of Health.
Ref 54 ClinicalTrials.gov (NCT00879333) Safety and Efficacy of RAD001 (Everolimus) Monotherapy Plus Best Supportive Care in Patients With Advanced Gastric Cancer (AGC) (GRANITE-1). U.S. National Institutes of Health.
Ref 55 ClinicalTrials.gov (NCT03504397) A Phase 3 Efficacy, Safety and Tolerability Study of Zolbetuximab (Experimental Drug) Plus mFOLFOX6 Chemotherapy Compared to Placebo Plus mFOLFOX6 as Treatment for Gastric and Gastroesophageal Junction (GEJ) Cancer (Spotlight). U.S. National Institutes of Health.
Ref 56 ClinicalTrials.gov (NCT05703555) INTRUSION: Unraveling the INTRatUmoral PK/PD relatION for SAR408701. U.S.National Institutes of Health.
Ref 57 ClinicalTrials.gov (NCT02545504) Andecaliximab With mFOLFOX6 as First Line Treatment for Advanced Gastric or Gastroesophageal Junction Adenocarcinoma (GAMMA-1). U.S. National Institutes of Health.
Ref 58 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 59 Clinical pipeline report, company report or official report of Taiho Pharma U.S.A.
Ref 60 Edotecarin: a novel topoisomerase I inhibitor. Clin Colorectal Cancer. 2005 May;5(1):27-36.
Ref 61 ClinicalTrials.gov (NCT02488330) An Extension Study of Onartuzumab in Patients With Solid Tumors on Study Treatment Previously Enrolled in a Company Sponsored Study.
Ref 62 ClinicalTrials.gov (NCT02118077) Sequential Trial of G17DT for the Treatment of Advanced Pancreatic Cancer. U.S. National Institutes of Health.
Ref 63 Clinical pipeline report, company report or official report of Daiichi Sankyo.
Ref 64 ClinicalTrials.gov (NCT01221870) Tesetaxel as First-line Therapy for Metastatic Breast Cancer. U.S. National Institutes of Health.
Ref 65 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
Ref 66 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800031678)
Ref 67 ClinicalTrials.gov (NCT05002127) A Phase 2/3 Study of Evorpacept (ALX148) in Patients With Advanced HER2-Overexpressing Gastric/Gastroesophageal Junction Adenocarcinoma (ASPEN-06). U.S.National Institutes of Health.
Ref 68 ClinicalTrials.gov (NCT04683939) Phase I/IIa, First-in-human, Open-label, Dose Escalation Trial With Expansion Cohorts to Evaluate Safety, Pharmacokinetics, Pharmacodynamics, and Preliminary Efficacy of BNT141 as a Monotherapy and in Combination With Other Anti-cancer Agents in Patients With CLDN18.2-positive Solid Tumors. U.S.National Institutes of Health.
Ref 69 ClinicalTrials.gov (NCT01218204) A Study to Investigate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Administering Multiple Oral Doses of GSK1292263 Alone and With Atorvastatin.U.S. National Institutes of Health.
Ref 70 ClinicalTrials.gov (NCT01774851) A Study of MM-111 and Paclitaxel With Trastuzumab in Patients HER2 Positive Carcinomas of the Distal Esophagus, Gastroesophageal (GE) Junction and Stomach. U.S. National Institutes of Health.
Ref 71 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8278).
Ref 72 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 5679).
Ref 73 ClinicalTrials.gov (NCT00073541) A Study of the Safety and Effects of EMD 72000 in Subjects With Recurrent Ovarian Cancer. U.S. National Institutes of Health.
Ref 74 ClinicalTrials.gov (NCT03694522) A Study of Bemarituzumab (FPA144) Combined With Modified FOLFOX6 (mFOLFOX6) in Gastric/Gastroesophageal Junction Cancer (FIGHT) (FIGHT). U.S. National Institutes of Health.
Ref 75 Clinical pipeline report, company report or official report of plevitrexed.
Ref 76 ClinicalTrials.gov (NCT04383938) Phase 1/2 Study of APR-246 in Combination With Pembrolizumab in Subjects With Solid Tumor Malignancies. U.S. National Institutes of Health.
Ref 77 ClinicalTrials.gov (NCT04404595) Open-label, Multicenter, Phase 1b/2 Clinical Trial to Evaluate the Safety and Efficacy of Autologous Anti-claudin 18.2 Chimeric Antigen Receptor T-cell Therapy in Subjects With Advanced Gastric, Pancreatic, or Other Specified Digestive System Cancers. U.S.National Institutes of Health.
Ref 78 ClinicalTrials.gov (NCT02744287) Use of Ligand-Inducible Autologous T Cells Engineered to Target PSCA on Tumor Cells in Selected Advanced Solid Tumors
Ref 79 ClinicalTrials.gov (NCT02617134) CAR-T Cell Immunotherapy in MUC1 Positive Solid Tumor
Ref 80 ClinicalTrials.gov (NCT03638206) Autologous CAR-T/TCR-T Cell Immunotherapy for Malignancies
Ref 81 ClinicalTrials.gov (NCT02713984) A Clinical Research of CAR T Cells Targeting HER2 Positive Cancer
Ref 82 ClinicalTrials.gov (NCT03013712) A Clinical Research of CAR T Cells Targeting EpCAM Positive Cancer
Ref 83 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800013314)
Ref 84 ClinicalTrials.gov (NCT05365581) A Phase 1/1b Study of ASP2138 in Participants With Metastatic or Locally Advanced Unresectable Gastric or Gastroesophageal Junction (GEJ) Adenocarcinoma or Metastatic Pancreatic Adenocarcinoma Whose Tumors Have Claudin (CLDN) 18.2 Expression. U.S.National Institutes of Health.
Ref 85 Clinical pipeline report, company report or official report of Sanofi
Ref 86 ClinicalTrials.gov (NCT04117958) Study of AMG 199 in Subjects With MUC17-Positive Gastric and Gastroesophageal Junction Cancer. U.S. National Institutes of Health.
Ref 87 ClinicalTrials.gov (NCT04260191) Study of AMG 910 in Subjects With CLDN18.2-Positive Gastric and Gastroesophageal Junction Adenocarcinoma. U.S. National Institutes of Health.
Ref 88 ClinicalTrials.gov (NCT04071184) Study of Alofanib in Patients With Metastatic Gastric Cancer. U.S. National Institutes of Health.
Ref 89 ClinicalTrials.gov (NCT03500991) HER2-specific CAR T Cell Locoregional Immunotherapy for HER2-positive Recurrent/Refractory Pediatric CNS Tumors
Ref 90 ClinicalTrials.gov (NCT02349724) A Clinical Research of CAR T Cells Targeting CEA Positive Cancer
Ref 91 Antitumor activity of XR5944, a novel and potent topoisomerase poison. Anticancer Drugs. 2001 Apr;12(4):359-67.
Ref 92 Clinical pipeline report, company report or official report of Klus Pharma
Ref 93 ClinicalTrials.gov (NCT03638167) EGFR806-specific CAR T Cell Locoregional Immunotherapy for EGFR-positive Recurrent or Refractory Pediatric CNS Tumors
Ref 94 ClinicalTrials.gov (NCT03563326) Intraperitoneal Infusion of EpCAM CAR-T Cell in Advanced Gastric Cancer With Peritoneal Metastasis (WCH-GC-CART)
Ref 95 ClinicalTrials.gov (NCT03682744) CAR-T Intraperitoneal Infusions for CEA-Expressing Adenocarcinoma Peritoneal Metastases or Malignant Ascites (IPC)
Ref 96 ClinicalTrials.gov (NCT02725125) Study Evaluating the Efficacy and Safety With CAR-T for Stomach Cancer
Ref 97 Cancer stem cell (CSC) inhibitors: a review of recent patents (2012-2015). Expert Opin Ther Pat. 2017 Jul;27(7):753-761. doi: 10.1080/13543776.2017.1325465. Epub 2017 May 5.
Ref 98 VEGFR-2 inhibitors and the therapeutic applications thereof: a patent review (2012-2016). Expert Opin Ther Pat. 2017 Sep;27(9):987-1004. doi: 10.1080/13543776.2017.1344215. Epub 2017 Jun 23.
Ref 99 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800015071)
Ref 100 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002544)
Ref 101 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007244)
Ref 102 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026781)
Ref 103 The ChEMBL database in 2017. Nucleic Acids Res. 2017 Jan 4;45(D1):D945-D954.