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Bromodomain-containing protein 3 Inhibitors (IC50, Ki)

Structure
Compound Name
Standard Type
Standard Values (in nM)
Tert-butyl 2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetateIC5039.1 [1], 56.7 [2], 69.0 [3], 81.0 [4]
Tert-butyl 2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetateKi6.6 [1], 8.9 [2]
MolibresibIC5042.4 [1], 160.0 [2], 390.0 [3], 400.0 [4]
MolibresibKi30.3 [1], 53.9 [2]
BirabresibIC5021.0 [1], 38.5 [2], 92.0 [3]
BirabresibKi4.0 [1], 10.7 [2]
I-Bet151 (gsk1210151A)IC50250.0 [1], 251.19 [2]
I-Bet151 (gsk1210151A)Ki7.2 [1], 22.3 [2]
4-[(2s,4r)-1-Acetyl-4-[(4-Chlorophenyl)amino]-2-Methyl-1,2,3,4-Tetrahydroquinolin-6-Yl]benzoic AcidIC500.25 [1], 0.63 [2], 2.0 [3], 199.53 [4]
ApabetaloneIC50203.0 [1], 510.0 [2], 3962.0 [3]
Tert-butyl 2-[7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetateIC5019.1 [1], 39.0 [2], 59.0 [3]
Benzyl [(4r)-1-Methyl-6-Phenyl-4h-[1,2,4]triazolo[4,3-A][1,4]benzodiazepin-4-Yl]carbamateIC5028.4 [1], 220.0 [2], 350.0 [3]
4-[(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-pyridin-2-ylbenzenesulfonamideKi100.0 [1], 140.0 [2]
8-[[(3R,4R)-3-[(1,1-Dioxothian-4-yl)methoxy]piperidin-4-yl]amino]-3-methyl-5-(5-methylpyridin-3-yl)-1H-1,7-naphthyridin-2-oneIC5050118.72 [1]
4-[(2-Amino-3-chloro-4-hydroxy-5-methylphenyl)diazenyl]-N-pyridin-2-ylbenzenesulfonamideKi240.0 [1], 320.0 [2]
1-[1-(Pyridin-2-Yl)indolizin-3-Yl]ethan-1-OneIC502500.0 [1], 6300.0 [2]
4-[1-(3-Cyclopropyl-5-methyl-1H-pyrazol-4-yl)-8-methoxy-5H-pyrido[4,3-b]indol-7-yl]-3,5-dimethyl-1,2-oxazoleKi3.2 [1], 7.3 [2]
5-(5-Methoxypyridin-3-Yl)-3-Methyl-8-[(Piperidin-4-Yl)amino]-1,2-Dihydro-1,7-Naphthyridin-2-OneIC506309.57 [1], 19952.62 [2]
3-Methyl-5-(5-methylpyridin-3-yl)-8-(piperidin-4-ylamino)-1H-1,7-naphthyridin-2-oneIC507943.28 [1], 19952.62 [2]
3-[(4-Chlorophenyl)methyl]-7-Ethyl-Purine-2,6-DioneIC501800.0 [1]
4-[1-(5-Ethyl-3-phenyl-1H-pyrazol-4-yl)-8-methoxy-5H-pyrido[4,3-b]indol-7-yl]-3,5-dimethyl-1,2-oxazoleKi9.4 [1], 10.4 [2]
8-[[(3R,4R)-3-[(1,1-Dioxothian-4-yl)methoxy]-1-methylpiperidin-4-yl]amino]-3-methyl-5-(5-methylpyridin-3-yl)-1H-1,7-naphthyridin-2-oneIC5050118.72 [1]
3-Butyl-7-ethylpurine-2,6-dioneIC504800.0 [1], 5800.0 [2]
4-[(5-Cyclopropyl-2-ethylpyrazol-3-yl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)-6-methoxy-N-methyl-9H-pyrimido[4,5-b]indole-2-carboxamideIC506.6 [1]
4-[(5-Cyclopropyl-2-ethylpyrazol-3-yl)amino]-7-(3,5-dimethyl-1,2-oxazol-4-yl)-6-methoxy-N-methyl-9H-pyrimido[4,5-b]indole-2-carboxamideKi0.21 [1]
4-[(E)-(4-Hydroxy-3,5-Dimethylphenyl)diazenyl]-N-(Pyridin-2-Yl)benzenesulfonamideKi1640.0 [1], 2480.0 [2]
4-[(E)-(2-Amino-4-Hydroxy-3,5-Dimethylphenyl)diazenyl]-N-(Pyridin-2-Yl)benzenesulfonamideKi220.0 [1], 290.0 [2]
5-(4-Hydroxy-3,5-dimethylphenyl)-11-methyl-8-thia-4,6,11-triazatricyclo[7.4.0.02,7]trideca-1(9),2(7),5-trien-3-oneIC50100000.0 [1]
4-[(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-cyclopentylbenzenesulfonamideIC502241.0 [1], 2493.0 [2]
6-[(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-3,4-dihydro-1H-quinolin-2-oneIC502193.0 [1], 2275.0 [2]
5-[(2S)-1-Acetyl-2-cyclopropyl-4-[[2-(hydroxymethyl)phenyl]methyl]-2,3-dihydroquinoxalin-6-yl]pyrimidine-2-carboxamideIC5031.62 [1], 794.33 [2]
1-[(2S)-2-Cyclopropyl-4-[[2-(hydroxymethyl)phenyl]methyl]-6-(1,2,3,6-tetrahydropyridin-4-yl)-2,3-dihydroquinoxalin-1-yl]ethanoneIC5050.12 [1], 1258.93 [2]
7-(3,5-Dimethyl-1,2-oxazol-4-yl)-6-methoxy-N-methyl-9H-pyrimido[4,5-b]indole-2-carboxamideIC50294.0 [1]
7-(3,5-Dimethyl-1,2-oxazol-4-yl)-6-methoxy-N-methyl-9H-pyrimido[4,5-b]indole-2-carboxamideKi42.4 [1]
N-Cyclopentyl-5-(3,5-dimethyl-1,2-oxazol-4-yl)-2-methoxybenzenesulfonamideIC50200.0 [1], 1000.0 [2]
N-Cyclopentyl-5-(3,5-Dimethylisoxazol-4-Yl)-2-MethylbenzenesulfonamideIC50250.0 [1], 500.0 [2]
4-[1-(3,5-Diethyl-1H-pyrazol-4-yl)-8-methoxy-5H-pyrido[4,3-b]indol-7-yl]-3,5-dimethyl-1,2-oxazoleKi4.2 [1], 12.9 [2]
2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-oneIC5013700.0 [1]
2-Piperazinyl-8-phenyl-4H-1-benzopyran-4-oneIC5011500.0 [1]
MivebresibKi12.2 [1]
Benzyl N-(1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl)carbamateIC50630.96 [1]
4-[(2-Tert-Butylphenyl)amino]-7-(3,5-Dimethyl-1,2-Oxazol-4-Yl)quinoline-3-Carboxylic AcidIC50501.19 [1]
5-(2-Amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-tert-butylpyridine-3-sulfonamideIC5010000.0 [1]
7-(3,5-Dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-(pyridin-2-ylmethyl)-3H-imidazo[4,5-c]quinolin-2-oneIC50501.19 [1]
7-(3,5-Dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-[(1R)-1-phenylethyl]-3H-imidazo[4,5-c]quinolin-2-oneIC50199.53 [1]
7-(3,5-Dimethyl-1,2-oxazol-4-yl)-1-(2-fluorophenyl)-8-methoxy-3H-imidazo[4,5-c]quinolin-2-oneIC50630.96 [1]
7-(3,5-Dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-[(1S)-1-phenylethyl]-3H-imidazo[4,5-c]quinolin-2-oneIC50630.96 [1]
7-(3,5-Dimethyl-1,2-oxazol-4-yl)-4-(2-fluoroanilino)quinoline-3-carboxamideIC503162.28 [1]
7-(3,5-Dimethyl-1,2-oxazol-4-yl)-4-(2-fluoroanilino)-6-methoxyquinoline-3-carboxamideIC50316.23 [1]
7-(3,5-Dimethyl-1,2-oxazol-4-yl)-6-methoxy-4-(quinolin-8-ylamino)quinoline-3-carboxamideIC50501.19 [1]
1-(2-Tert-butylphenyl)-7-(3,5-dimethyl-1,2-oxazol-4-yl)-8-methoxy-3H-imidazo[4,5-c]quinolin-2-oneIC50398.11 [1]
4-(Cyclohexylamino)-7-(3,5-dimethyl-1,2-oxazol-4-yl)-6-methoxyquinoline-3-carboxamideIC50501.19 [1]
1-Benzyl-7-(3,5-dimethyl-1,2-oxazol-4-yl)-8-methoxy-3H-imidazo[4,5-c]quinolin-2-oneIC50251.19 [1]
N-[3-(3-Methyl-4-Oxo-4,5,6,7-Tetrahydro-2h-Isoindol-1-Yl)-4-Phenoxyphenyl]methanesulfonamideKi35.0 [1]
1-[2-(2,4-Difluorophenoxy)-5-methylsulfonylphenyl]-3-methyl-2,5,6,7-tetrahydropyrrolo[3,4-c]pyridin-4-oneKi110.0 [1]
N'-(1,1-Dioxothian-4-yl)-5-ethyl-4-oxo-7-[3-(trifluoromethyl)phenyl]thieno[3,2-c]pyridine-2-carboximidamideIC5050118.72 [1]
1-[(2S,4R)-4-Anilino-2-methyl-6-phenyl-3,4-dihydro-2H-quinolin-1-yl]ethanoneIC50501.19 [1]
4-[(2S,4R)-1-Acetyl-4-anilino-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzonitrileIC50794.33 [1]
1-[(2S,4R)-4-Anilino-2-methyl-6-[4-(trifluoromethyl)phenyl]-3,4-dihydro-2H-quinolin-1-yl]ethanoneIC501258.93 [1]
1-[(2S,4R)-4-Anilino-6-(4-methoxyphenyl)-2-methyl-3,4-dihydro-2H-quinolin-1-yl]ethanoneIC50630.96 [1]
1-[(2S,4R)-4-Anilino-6-[4-(hydroxymethyl)phenyl]-2-methyl-3,4-dihydro-2H-quinolin-1-yl]ethanoneIC50501.19 [1]
1-[(2S,4R)-4-Anilino-2-methyl-6-[4-(morpholin-4-ylmethyl)phenyl]-3,4-dihydro-2H-quinolin-1-yl]ethanoneIC50630.96 [1]
1-[(2S,4R)-4-Anilino-2-methyl-6-[3-(piperidin-1-ylmethyl)phenyl]-3,4-dihydro-2H-quinolin-1-yl]ethanoneIC50398.11 [1]
1-[(2R,4S)-4-Anilino-2-methyl-6-[4-(piperidin-1-ylmethyl)phenyl]-3,4-dihydro-2H-quinolin-1-yl]ethanoneIC5025118.86 [1]
Methyl 4-[(2S,4R)-1-acetyl-4-(4-tert-butylanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoateIC50501.19 [1]
4-[(2S,4R)-1-Acetyl-2-methyl-4-(4-methylsulfonylanilino)-3,4-dihydro-2H-quinolin-6-yl]benzoic acidIC50316.23 [1]
Methyl 4-[(2S,4R)-1-acetyl-2-methyl-4-(4-methylsulfonylanilino)-3,4-dihydro-2H-quinolin-6-yl]benzoateIC50501.19 [1]
Methyl 4-[(2S,4R)-1-acetyl-4-(4-fluoroanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoateIC501000.0 [1]
4-[(2S,4R)-1-Acetyl-4-(3-fluoroanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzonitrileIC50794.33 [1]
4-[(2S,4R)-1-Acetyl-4-(3-methoxyanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzonitrileIC50794.33 [1]
4-[(2S,4R)-1-Acetyl-4-(3-methoxyanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoic acidIC50501.19 [1]
4-[(2S,4R)-1-Acetyl-4-(2-methoxyanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoic acidIC50501.19 [1]
1-[(2S,4R)-4-(4-Chloroanilino)-2-methyl-6-[4-(piperidin-1-ylmethyl)phenyl]-3,4-dihydro-2H-quinolin-1-yl]ethanoneIC501258.93 [1]
3-[(2S,4R)-1-Acetyl-4-(4-chloroanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoic acidIC50501.19 [1]
Methyl 3-[(2S,4R)-1-acetyl-4-(4-chloroanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoateIC501000.0 [1]
1-[(2S,4R)-4-(4-Chloroanilino)-2-methyl-6-(2-methylphenyl)-3,4-dihydro-2H-quinolin-1-yl]ethanoneIC502511.89 [1]
1-[(4R)-4-Anilino-6-(4-methoxyphenyl)-3,4-dihydro-2H-quinolin-1-yl]ethanoneIC501584.89 [1]
7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepineIC5025.0 [1]
Methyl 7-(4-chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxylateIC5018.0 [1]
7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxylic acidIC5016.0 [1]
7-(4-Chlorophenyl)-1-methyl-9-(1H-pyrazol-5-yl)-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepineIC5010.0 [1]
5-[7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepin-9-yl]pyrimidin-2-amineIC5014.0 [1]
(5S)-7-(4-Chlorophenyl)-1,5-dimethyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepineIC5013.0 [1]
(5R)-7-(4-Chlorophenyl)-1,5-dimethyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepineIC5011.0 [1]
N-Benzhydryl-7-(4-chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamideIC5039.0 [1]
7-(4-Chlorophenyl)-N-[(1S)-1-(4-fluorophenyl)ethyl]-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamideIC5023.0 [1]
2-[7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepin-5-yl]ethanolIC5044.0 [1]
[7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepin-9-yl]methanolIC5036.0 [1]
7-(4-Chlorophenyl)-1-methyl-9-(6-methylpyridin-3-yl)-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepineIC5010.0 [1]
1-Methyl-7-phenyl-5H-triazolo[1,5-d][1,4]benzodiazepin-6-oneIC5010000.0 [1]
5-[7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepin-9-yl]pyridin-2-amineIC509.0 [1]
1-Methyl-7-phenyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepineIC5019.0 [1]
N-(Benzenesulfonyl)-7-(4-chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamideIC5021.0 [1]
7-(4-Chlorophenyl)-1-methyl-N-phenyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamideIC5014.0 [1]
N-Benzyl-7-(4-chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamideIC5021.0 [1]
7-(4-Chlorophenyl)-1-methyl-N-[(1S)-1-phenylethyl]-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamideIC5012.0 [1]
7-(4-Chlorophenyl)-1-methyl-N-[(1R)-1-phenylethyl]-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamideIC5013.0 [1]
8-[(5-Amino-1H-1,2,4-triazol-3-yl)sulfanylmethyl]-3-[(4-chlorophenyl)methyl]-7-ethylpurine-2,6-dioneIC5031700.0 [1]
7-(4-Chlorophenyl)-1-methyl-9-(pyrazol-1-ylmethyl)-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepineIC5052.0 [1]
1-Methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-amineIC5012589.25 [1]



References

This online tool may be cited as follows

MLA

"Quest Database™ Bromodomain-containing protein 3 Inhibitors (IC50, Ki)." AAT Bioquest, Inc.10 May2024https://www.aatbio.com/data-sets/bromodomain-containing-protein-3-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024May 10). Quest Database™ Bromodomain-containing protein 3 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/bromodomain-containing-protein-3-inhibitors-ic50-ki.
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