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Tankyrase-1 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
3,5,7,8-Tetrahydro-2-[4-(trifluoromethyl)phenyl]-4H-thiopyrano[4,3-d]pyrimidin-4-oneIC5011.1 [1]
OlaparibIC501230.27 [1], 1500.0 [2], 1800.0 [3], 1900.0 [4], 3534.0 [5]
(4S)-3-[4-(6-Amino-5-pyrimidin-2-ylpyridin-3-yl)cyclohexyl]-5,5-dimethyl-4-phenyl-1,3-oxazolidin-2-oneIC501.47 [1], 2.0 [2], 370.0 [3]
N~2~,N~2~-Dimethyl-N~1~-(6-oxo-5,6-dihydrophenanthridin-2-YL)glycinamideIC50570.0 [1], 1300.0 [2], 1698.24 [3]
IWR-1-endoIC50131.0 [1], 150.0 [2], 151.0 [3]
4-[(4S)-5,5-Dimethyl-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]-N-quinolin-8-ylcyclohexane-1-carboxamideIC5016.0 [1], 16.8 [2], 5200.0 [3]
[4-(1-Methylimidazole-4-carbonyl)piperazin-1-yl]-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanoneIC502.51 [1], 31.62 [2]
(4-Pyrimidin-2-ylpiperazin-1-yl)-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanoneIC507.94 [1], 15.85 [2], 19.95 [3]
3-(4-(Dimethylaminomethyl)phenyl)isoquinoline-1(2H)-oneIC5018.0 [1], 10000.0 [2]
3-(4-(Dimethylaminomethyl)phenyl)-5-methylisoquinoline-1(2H)-oneIC5012.0 [1], 72.0 [2]
FlavoneIC50320.0 [1], 330.0 [2]
VeliparibIC5010000.0 [1], 10715.19 [2]
RucaparibIC5025.0 [1], 144.54 [2]
NiraparibIC50570.0 [1], 2344.23 [2]
4H-Thieno[2,3-c]isoquinolin-5-oneIC50200.0 [1], 100000.0 [2]
2-Phenylquinazolin-4-olIC5059.0 [1], 1406.0 [2]
4'-FluoroflavoneIC50280.0 [1], 700.0 [2]
2-(4-Chlorophenyl)quinazolin-4-olIC50140.0 [1], 485.0 [2]
N-Phenyltetrazolo[1,5-a]quinoxalin-4-amineIC50251.19 [1], 1995.26 [2]
4,4'-OxydibenzamideIC50100000.0 [1]
2-(4-Methylphenyl)-4H-chromen-4-oneIC5047.0 [1], 52.0 [2]
N-(3-Methylphenyl)-4-tetrazolo[1,5-a]quinoxalinamineIC5010000.0 [1], 15848.93 [2]
N-(4-Chlorophenyl)tetrazolo[1,5-a]quinoxalin-4-amineIC50398.11 [1], 1258.93 [2]
N-(4-Methylphenyl)-4-tetrazolo[1,5-a]quinoxalinamineIC50125.89 [1], 1258.93 [2]
Morpholin-4-Yl[4-(Tetrazolo[1,5-A]quinoxalin-4-Ylamino)phenyl]methanoneIC5050.12 [1], 158.49 [2]
4-[(1R,2S,6R,7S)-3,5-Dioxo-4-azatricyclo[5.2.1.02,6]dec-8-en-4-yl]-N-(4-methylquinolin-8-yl)benzamideIC50160.0 [1], 192.0 [2]
5H-Benzothiopheno[2,3-c]quinolin-6-oneIC5090.0 [1]
N-(2-Methoxyphenyl)-4-{[3-(4-Oxo-3,4-Dihydroquinazolin-2-Yl)propanoyl]amino}benzamideIC508.0 [1], 10.0 [2]
2-[4-(Trifluoromethyl)phenyl]-3h-Quinazolin-4-OneIC5050.0 [1], 425.0 [2]
2-[4-(Trifluoromethyl)phenyl]-3,5,6,8-tetrahydrothiopyrano[3,4-d]pyrimidin-4-oneIC5011.0 [1], 5000.0 [2]
4-N,4-N-Dimethyl-1-N-(tetrazolo[1,5-a]quinoxalin-4-yl)benzene-1,4-diamineIC5063.1 [1], 1258.93 [2]
N-(2-Methoxyphenyl)-4-[3-(4-oxo-3H-quinazolin-2-yl)propanoylamino]cyclohexane-1-carboxamideIC5031.0 [1], 7460.0 [2]
[4-(Oxan-4-yl)piperazin-1-yl]-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanoneIC5031.62 [1], 251.19 [2]
Morpholin-4-yl-[3-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanoneIC5010000.0 [1]
N-(3-Propan-2-ylphenyl)tetrazolo[1,5-a]quinoxalin-4-amineIC5010000.0 [1], 199526.23 [2]
[3-Fluoro-4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]-morpholin-4-ylmethanoneIC507943.28 [1], 10000.0 [2]
N-(2-Methylphenyl)tetrazolo[1,5-a]quinoxalin-4-amineIC5010000.0 [1], 63095.73 [2]
(4-Pyrimidin-4-ylpiperazin-1-yl)-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanoneIC502.0 [1], 6.31 [2]
N-(4-Propan-2-ylphenyl)tetrazolo[1,5-a]quinoxalin-4-amineIC50125.89 [1], 199.53 [2]
(4-Pyridin-2-ylpiperazin-1-yl)-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanoneIC5031.62 [1], 100.0 [2]
N-(4-Fluorophenyl)tetrazolo[1,5-a]quinoxalin-4-amineIC50630.96 [1], 3981.07 [2]
N-[4-(Tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]acetamideIC5019.95 [1], 251.19 [2]
4-[(4s)-5,5-Dimethyl-2-Oxo-4-Phenyl-1,3-Oxazolidin-3-Yl]-N-(Quinolin-8-Yl)benzamideIC50198.0 [1], 200.0 [2]
4-[(4S)-5,5-Dimethyl-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]-N-(1,5-naphthyridin-4-yl)benzamideIC5018.0 [1], 18.3 [2]
N-[4-[(4S)-5,5-Dimethyl-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]cyclohexyl]quinoline-8-carboxamideIC5010.0 [1], 22.0 [2]
N-[4-[(4S)-5,5-Dimethyl-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]cyclohexyl]-1,5-naphthyridine-4-carboxamideIC504.0 [1], 4.56 [2]
N-[4-[(4S)-5,5-Dimethyl-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]cyclohexyl]-7-fluoro-1,5-naphthyridine-4-carboxamideIC503.86 [1], 4.0 [2]
(4S)-5,5-Dimethyl-3-[4-(2-oxo-3H-imidazo[4,5-c]pyridin-1-yl)cyclohexyl]-4-phenyl-1,3-oxazolidin-2-oneIC503.0 [1], 3.04 [2]
(4S)-5,5-Dimethyl-3-[4-(2-oxo-3H-imidazo[4,5-b]pyridin-1-yl)cyclohexyl]-4-phenyl-1,3-oxazolidin-2-oneIC5010.7 [1], 11.0 [2]
1-[4-[(4S)-5,5-Dimethyl-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]cyclohexyl]-2-oxo-3H-benzimidazole-5-carbonitrileIC501.0 [1], 1.12 [2]
1-[4-[(4S)-5,5-Dimethyl-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]cyclohexyl]-2-oxo-3H-benzimidazole-4-carbonitrileIC503.56 [1], 4.0 [2]
1-[4-[(4S)-5,5-Dimethyl-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]cyclohexyl]-6-fluoro-2-oxo-3H-benzimidazole-5-carbonitrileIC503.0 [1], 3.48 [2]
1-[4-[(4S)-5,5-Dimethyl-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]cyclohexyl]-4-fluoro-2-oxo-3H-benzimidazole-5-carbonitrileIC501.0 [1], 1.09 [2]
3-[4-[(4S)-5,5-Dimethyl-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]cyclohexyl]-2-oxo-1H-imidazo[4,5-b]pyridine-6-carbonitrileIC50143.0 [1]
(4S)-5,5-Dimethyl-3-[4-(2-oxo-1H-imidazo[4,5-b]pyridin-3-yl)cyclohexyl]-4-phenyl-1,3-oxazolidin-2-oneIC504.0 [1], 11.8 [2]
(4S)-5,5-Dimethyl-3-[4-(2-oxo-1H-imidazo[4,5-c]pyridin-3-yl)cyclohexyl]-4-phenyl-1,3-oxazolidin-2-oneIC504.0 [1], 4.07 [2]
(4S)-5,5-Dimethyl-3-[4-(8-oxo-7H-purin-9-yl)cyclohexyl]-4-phenyl-1,3-oxazolidin-2-oneIC505.0 [1], 5.11 [2]
(4s)-3-{4-[6-Amino-5-(Pyrimidin-2-Yl)pyridin-3-Yl]phenyl}-5,5-Dimethyl-4-Phenyl-1,3-Oxazolidin-2-OneIC5049.0 [1]
4-[[1-[[2-Cyano-3-(trifluoromethyl)phenyl]methyl]-2,4-dioxoquinazolin-3-yl]methyl]cyclohexane-1-carboxylic acidIC507.94 [1], 31.62 [2]
4-[[1-[[2-Cyano-3-(trifluoromethyl)phenyl]methyl]-6-fluoro-5-methyl-2,4-dioxoquinazolin-3-yl]methyl]cyclohexane-1-carboxylic acidIC506.31 [1], 50.12 [2]
2-Amino-5-[4-[(4S)-5,5-dimethyl-2-oxo-4-phenyl-1,3-oxazolidin-3-yl]cyclohexyl]pyridine-3-carbonitrileIC506.98 [1], 9.0 [2]
Cyclopropyl-[4-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)benzoyl]piperazin-1-yl]methanoneIC5019.95 [1], 5011.87 [2]
[4-(1H-Pyrazole-5-carbonyl)piperazin-1-yl]-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanoneIC5010.0 [1], 125.89 [2]
[4-(3-Methylimidazole-4-carbonyl)piperazin-1-yl]-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanoneIC5025.12 [1], 398.11 [2]
[4-(1H-Imidazole-5-carbonyl)piperazin-1-yl]-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanoneIC503.98 [1], 251.19 [2]
1-[4-[4-(Tetrazolo[1,5-a]quinoxalin-4-ylamino)benzoyl]piperazin-1-yl]ethanoneIC5015.85 [1], 125.89 [2]
(4-Pyridin-3-ylpiperazin-1-yl)-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanoneIC5025.12 [1], 63.1 [2]
Tnks-IN-41IC507.94 [1], 100.0 [2]
[4-(Pyrimidine-2-carbonyl)piperazin-1-yl]-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanoneIC5015.85 [1], 398.11 [2]
N-(2-Methoxyethyl)-4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)benzamideIC50199.53 [1], 630.96 [2]
(4-Pyridin-4-ylpiperazin-1-yl)-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanoneIC506.31 [1], 125.89 [2]
4-(Tetrazolo[1,5-a]quinoxalin-4-ylamino)benzoic acidIC50398.11 [1], 10000.0 [2]
Piperazin-1-yl-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanoneIC5050.12 [1], 794.33 [2]
N-(2-Methoxyethyl)-N-methyl-4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)benzamideIC5019.95 [1], 79.43 [2]
1-[4-(Tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]pyrrolidin-2-oneIC507.94 [1], 100.0 [2]
4-[4-(Tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]morpholin-3-oneIC507.94 [1], 100.0 [2]
N-Methyl-N-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]acetamideIC5010.0 [1], 79.43 [2]
Piperidin-1-yl-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)phenyl]methanoneIC5063.1 [1], 501.19 [2]
Oxan-4-yl-[4-[4-(tetrazolo[1,5-a]quinoxalin-4-ylamino)benzoyl]piperazin-1-yl]methanoneIC5025.12 [1], 199.53 [2]
3-(4-(3-(Dimethylamino)azetidine-1-ylmethyl)phenyl)-5-methylisoquinoline-1(2H)-oneIC5021.0 [1], 35.0 [2]
3-(4-(Trifluoromethyl)phenyl)-5-chloroisoquinoline-1(2H)-oneIC50128.0 [1], 483.0 [2]
3-(4-Fluorophenyl)-5-methoxyisoquinoline-1(2H)-oneIC50104.0 [1], 120.0 [2]
3-(4-(Dimethylaminomethyl)phenyl)-5-chloroisoquinoline-1(2H)-oneIC50151.0 [1], 364.0 [2]
3-(4-(Dimethylaminomethyl)phenyl)-5-fluoroisoquinoline-1(2H)-oneIC5016.0 [1], 1730.0 [2]
3-(4-(Morpholinomethyl)phenyl)-5-methylisoquinoline-1(2H)-oneIC5012.0 [1], 25.0 [2]
3-(4-(4-Methylpiperazinomethyl)phenyl)-5-methylisoquinoline-1(2H)-oneIC5017.0 [1], 43.0 [2]
3-(4-{[4-(Dimethylamino)piperidin-1-Yl]methyl}phenyl)-5-Methylisoquinolin-1(2h)-OneIC5013.0 [1], 61.0 [2]
5-Methyl-3-[4-(Piperazin-1-Ylmethyl)phenyl]isoquinolin-1(2h)-OneIC5017.0 [1], 117.0 [2]
3-(4-Methylphenyl)-5-methoxyisoquinoline-1(2H)-oneIC5034.0 [1], 59.0 [2]
(4S)-5,5-Dimethyl-3-[4-(6-oxo-5-pyrimidin-2-yl-1H-pyridin-3-yl)cyclohexyl]-4-phenyl-1,3-oxazolidin-2-oneIC50267.0 [1], 511.0 [2]
(4S)-3-[4-[6-Amino-5-(1,4,5,6-tetrahydropyrimidin-2-yl)pyridin-3-yl]cyclohexyl]-5,5-dimethyl-4-phenyl-1,3-oxazolidin-2-oneIC501650.0 [1], 9840.0 [2]
(4S)-5,5-Dimethyl-4-phenyl-3-[4-(1H-pyrrolo[3,2-b]pyridin-6-yl)cyclohexyl]-1,3-oxazolidin-2-oneIC5019.0 [1], 1250.0 [2]
3-{4-[(Dimethylamino)methyl]phenyl}-5-Methoxyisoquinolin-1(2h)-OneIC5019.0 [1], 136.0 [2]
ApigeninIC503100.0 [1]
LuteolinIC502400.0 [1]
6(5H)-PhenanthridinoneIC50110.0 [1]
Bmn-673 8R,9SIC50323.59 [1]
3',4'-DihydroxyflavoneIC50230.0 [1]
4'-MethoxyflavoneIC5071.0 [1]
7,3',4'-TrihydroxyflavoneIC50630.0 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Tankyrase-1 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.21 Nov2024https://www.aatbio.com/data-sets/tankyrase-1-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024November 21). Quest Database™ Tankyrase-1 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/tankyrase-1-inhibitors-ic50-ki.
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