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Bromodomain-containing protein 4 Inhibitors (IC50, Ki)

Structure
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Compound Name
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Standard Type
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Standard Values (in nM)
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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]acetateIC5077.0 [1]
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]acetateKi12.0 [1], 14.9 [2]
MolibresibIC50120.0 [1]
MolibresibKi23.0 [1], 32.3 [2], 38.8 [3], 46.4 [4]
ApabetaloneIC501985.0 [1]
I-Bet151 (gsk1210151A)IC50130.0 [1]
I-Bet151 (gsk1210151A)Ki9.0 [1], 74.8 [2]
BI-2536IC5025.0 [1]
BI-2536Ki56.0 [1]
MivebresibIC501.0 [1], 20.0 [2], 69.0 [3], 74.0 [4]
MivebresibKi1.4 [1], 1.5 [2], 3.5 [3], 15.0 [4]
BirabresibIC5016.0 [1], 16.6 [2], 20.0 [3], 92.0 [4]
BirabresibKi6.0 [1], 10.9 [2]
2-Methoxy-N-(3-Methyl-2-Oxo-1,2,3,4-Tetrahydroquinazolin-6-Yl)benzenesulfonamideIC50220.0 [1]
4-[(2s,4r)-1-Acetyl-4-[(4-Chlorophenyl)amino]-2-Methyl-1,2,3,4-Tetrahydroquinolin-6-Yl]benzoic AcidIC500.4 [1], 3.16 [2], 22.0 [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]acetateIC5035.0 [1]
6-(3,5-Dimethyl-1,2-oxazol-4-yl)-1-[[4-(oxiran-2-yl)phenyl]methyl]benzimidazol-4-amineIC5050.0 [1]
4-[(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-cyclopentylbenzenesulfonamideIC50730.0 [1]
6-[(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-3,4-dihydro-1H-quinolin-2-oneIC50490.0 [1]
1-Benzyl-6-(3,5-dimethyl-1,2-oxazol-4-yl)benzimidazol-4-amineIC5017.0 [1]
N-[3-(3-Methyl-4-Oxo-4,5,6,7-Tetrahydro-2h-Isoindol-1-Yl)-4-Phenoxyphenyl]methanesulfonamideKi15.0 [1], 18.0 [2], 33.0 [3], 38.0 [4], 43.0 [5]
CID 40642506IC504.7 [1], 10400.0 [2], 20000.0 [3], 50118.72 [4]
3-Methyl-8-[[(1R,5S)-8-methyl-8-azabicyclo[3.2.1]octan-3-yl]amino]-1H-1,7-naphthyridin-2-oneIC503162.28 [1], 3981.07 [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-oneIC505011.87 [1], 15848.93 [2]
1-[2-(2,4-Difluorophenoxy)-5-methylsulfonylphenyl]-3-methyl-2,5,6,7-tetrahydropyrrolo[3,4-c]pyridin-4-oneIC5035.0 [1]
1-[2-(2,4-Difluorophenoxy)-5-methylsulfonylphenyl]-3-methyl-2,5,6,7-tetrahydropyrrolo[3,4-c]pyridin-4-oneKi34.0 [1], 38.0 [2], 300.0 [3]
N-(Cyclopropylmethyl)-N-[4-(2,4-difluorophenoxy)-3-(4-ethoxy-1-methyl-6-oxopyridin-3-yl)phenyl]ethanesulfonamideIC502.3 [1], 61.0 [2]
N-(Cyclopropylmethyl)-N-[4-(2,4-difluorophenoxy)-3-(4-ethoxy-1-methyl-6-oxopyridin-3-yl)phenyl]ethanesulfonamideKi2.28 [1], 60.9 [2]
N-[4-(2,4-Difluorophenoxy)-3-(4-ethoxy-1-methyl-6-oxopyridin-3-yl)phenyl]-3-phenylpropanamideIC5011.0 [1], 69.0 [2]
N-[4-(2,4-Difluorophenoxy)-3-(4-ethoxy-1-methyl-6-oxopyridin-3-yl)phenyl]-3-phenylpropanamideKi10.8 [1], 68.5 [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-oneIC5079432.82 [1], 501187.23 [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-oneKi7943.28 [1]
2-(5-Tert-butyl-1,2-oxazol-3-yl)-5-(3-chloro-5-fluorophenyl)-1,3,4-oxadiazoleIC503900.0 [1], 4300.0 [2], 7700.0 [3], 7900.0 [4]
8-(4-Fluorophenyl)-12-methyl-4-(methylsulfonylmethyl)-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-oneIC502.5 [1]
8-(4-Fluorophenyl)-12-methyl-4-(methylsulfonylmethyl)-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-oneKi1.2 [1], 2.5 [2], 3.3 [3]
(R)-(-)-JQ1 EnantiomerIC508354000.0 [1], 10000000.0 [2], 52120000.0 [3]
15-Methyl-4-(methylsulfonylmethyl)-8-pyridin-2-yl-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-oneIC501.7 [1]
15-Methyl-4-(methylsulfonylmethyl)-8-pyridin-2-yl-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-oneKi0.62 [1], 1.2 [2], 1.5 [3]
8-(2,4-Difluorophenyl)-15-methyl-4-(methylsulfonylmethyl)-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-oneIC503.6 [1]
8-(2,4-Difluorophenyl)-15-methyl-4-(methylsulfonylmethyl)-8,12,15-triazatetracyclo[8.6.1.02,7.013,17]heptadeca-1(16),2(7),3,5,10,13(17)-hexaen-14-oneKi0.73 [1], 0.87 [2], 2.6 [3]
4-[2-(Cyclopropylmethylamino)-5-methylsulfonylphenyl]-6-methyl-1H-pyrrolo[2,3-c]pyridin-7-oneIC5020.0 [1]
4-[2-(Cyclopropylmethylamino)-5-methylsulfonylphenyl]-6-methyl-1H-pyrrolo[2,3-c]pyridin-7-oneKi8.9 [1], 12.6 [2], 13.0 [3]
4-[2-(Cyclopropylmethylamino)-5-(methylsulfonylmethyl)phenyl]-6-methyl-1H-pyrrolo[2,3-c]pyridin-7-oneIC5058.0 [1]
4-[2-(Cyclopropylmethylamino)-5-(methylsulfonylmethyl)phenyl]-6-methyl-1H-pyrrolo[2,3-c]pyridin-7-oneKi24.5 [1], 69.0 [2], 79.7 [3]
4-[2-(Cyclopropylmethylamino)phenyl]-6-methyl-1H-pyrrolo[2,3-c]pyridin-7-oneIC501900.0 [1]
4-[2-(Cyclopropylmethylamino)phenyl]-6-methyl-1H-pyrrolo[2,3-c]pyridin-7-oneKi404.0 [1], 625.0 [2], 680.0 [3]
4-[5-Ethylsulfonyl-2-(4-methoxycyclohexyl)oxyphenyl]-6-methyl-1H-pyrrolo[2,3-c]pyridin-7-oneKi1.0 [1], 1.2 [2], 1.3 [3], 1.9 [4]
4-[5-Ethylsulfonyl-2-(4-hydroxycyclohexyl)oxyphenyl]-6-methyl-1H-pyrrolo[2,3-c]pyridin-7-oneKi0.69 [1], 0.75 [2], 1.4 [3], 1.7 [4]
VorinostatIC5010.0 [1], 740.0 [2], 50000.0 [3]
4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)-1H-imidazoleIC502500.0 [1], 3400.0 [2]
CID 16722832IC50130.0 [1]
Sgc-cbp30IC503200.0 [1], 5850.0 [2], 20000.0 [3]
1-[7-(3,4-Dimethoxyphenyl)-9-[[(3S)-1-methylpiperidin-3-yl]methoxy]-3,5-dihydro-2H-1,4-benzoxazepin-4-yl]propan-1-oneIC50600.0 [1], 15000.0 [2]
4-[4-[(Dimethylamino)methyl]-2,5-Dimethoxy-Phenyl]-2-Methyl-2,7-Naphthyridin-1-OneIC50100000.0 [1]
Methyl 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]acetateIC5018.2 [1]
Methyl 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]acetateKi16.7 [1], 17.0 [2]
3,5 Dimethyl-4-Phenyl-1,2-OxazoleIC50800.0 [1], 65000.0 [2], 84200.0 [3]
4-[4-[(Dimethylamino)methyl]-3,5-Dimethoxy-Phenyl]-2-Methyl-2,7-Naphthyridin-1-OneIC50100000.0 [1]
CID 122705990IC5010000.0 [1], 15650.0 [2], 20000.0 [3]
Benzyl [(4r)-1-Methyl-6-Phenyl-4h-[1,2,4]triazolo[4,3-A][1,4]benzodiazepin-4-Yl]carbamateIC5015.5 [1], 140.0 [2], 470.0 [3]
CID 91827373IC503700.0 [1], 10000.0 [2], 33000.0 [3]
7-(3,5-Dimethyl-1,2-Oxazol-4-Yl)-6-Methoxy-2-Methyl-4-(Quinolin-4-Yl)-9h-Pyrimido[4,5-B]indoleIC5028.2 [1]
7-(3,5-Dimethyl-1,2-Oxazol-4-Yl)-6-Methoxy-2-Methyl-4-(Quinolin-4-Yl)-9h-Pyrimido[4,5-B]indoleKi1.4 [1], 8.2 [2]
CID 118021718IC502.0 [1], 5.0 [2], 100.0 [3]
4-Cyano-N-(1,3-dimethyl-2-oxoquinolin-6-yl)benzenesulfonamideIC504500.0 [1], 20000.0 [2]
4-Cyano-N-(1,3-diethyl-2-oxoquinolin-6-yl)benzenesulfonamideIC5020000.0 [1], 100000.0 [2]
3-[(3S)-3-Aminopiperidin-1-yl]-5-(3,5-dimethyl-1,2-oxazol-4-yl)-3-thiophen-3-yl-1H-indol-2-oneIC508.0 [1]
4-[6-Methoxy-2-methyl-4-(2-methyl-1H-indol-3-yl)-9H-pyrimido[4,5-b]indol-7-yl]-3,5-dimethyl-1,2-oxazoleIC506.1 [1]
4-[6-Methoxy-2-methyl-4-(2-methyl-1H-indol-3-yl)-9H-pyrimido[4,5-b]indol-7-yl]-3,5-dimethyl-1,2-oxazoleKi0.5 [1], 0.8 [2]
5-(3,5-Dimethyl-1,2-oxazol-4-yl)-1-[[4-(oxiran-2-yl)phenyl]methyl]pyridin-2-oneIC50160.0 [1], 470.0 [2], 480.0 [3]
6-(3-Hydroxypropyl)-2-(1-methyl-2-oxo-3H-benzimidazol-5-yl)benzo[de]isoquinoline-1,3-dioneIC5010000.0 [1], 20000.0 [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-oneIC50430.0 [1], 470.0 [2], 930.0 [3]
BET Inhibitor C3IC50900.0 [1], 1000.0 [2]
BET Inhibitor C3Ki370.0 [1]
N-[4-(2-Chloro-4-fluorophenoxy)-3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]methanesulfonamideKi2.1 [1], 3.1 [2], 3.5 [3]
N-[5-(6-Methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-6-phenoxypyridin-3-yl]methanesulfonamideKi0.75 [1], 1.2 [2], 4.1 [3]
N-[3-(6-Methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxyphenyl]ethanesulfonamideKi0.25 [1], 0.39 [2], 1.5 [3]
4-[5-(Dimethylsulfamoylamino)-2-phenoxyphenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridineKi1.0 [1], 2.2 [2], 2.9 [3]
3-(6-Methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxybenzamideKi4.2 [1], 7.4 [2], 14.0 [3]
6-Methyl-4-(2-Phenoxyphenyl)-1,6-Dihydro-7h-Pyrrolo[2,3-C]pyridin-7-OneKi41.0 [1], 48.0 [2], 136.0 [3]
N-[3-(6-Methyl-7-Oxo-6,7-Dihydro-1h-Pyrrolo[2,3-C]pyridin-4-Yl)-4-Phenoxyphenyl]methanesulfonamideKi1.4 [1], 2.0 [2], 2.4 [3]
2,2,2-Trifluoro-N-[3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxyphenyl]ethanesulfonamideKi4.4 [1], 6.4 [2], 15.0 [3]
N-[3-(6-Methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxyphenyl]acetamideKi5.3 [1], 5.8 [2], 9.8 [3]
N-Ethyl-3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxybenzamideKi3.4 [1], 3.7 [2], 32.0 [3]
N-[4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]methanesulfonamideKi2.2 [1], 2.5 [2], 4.5 [3]
N-[3-(6-Methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(oxan-4-yloxy)phenyl]methanesulfonamideKi1.1 [1], 6.7 [2], 68.0 [3]
3-(6-Methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenoxybenzenesulfonamideKi1.1 [1], 3.6 [2], 8.7 [3]
N-[4-(4-Cyanophenoxy)-3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethanesulfonamideKi4.0 [1], 6.8 [2], 9.4 [3]
6-Methyl-4-(5-methylsulfonyl-2-phenoxyphenyl)-1H-pyrrolo[2,3-c]pyridin-7-oneKi1.7 [1], 5.8 [2], 6.4 [3]
N-[3-(6-Methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-phenylmethoxyphenyl]methanesulfonamideKi18.0 [1], 42.7 [2], 68.0 [3]
N-[3-(6-Methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-(2,4,6-trifluorophenoxy)phenyl]ethanesulfonamideKi1.9 [1], 3.0 [2], 12.0 [3]
N-[4-(4,4-Difluorocyclohexyl)oxy-3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]methanesulfonamideKi0.84 [1], 1.6 [2], 19.0 [3]
N-[4-Cyclohexyloxy-3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]methanesulfonamideKi0.88 [1], 2.0 [2], 3.7 [3]
N-[3-(6-Methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-pyridin-3-yloxyphenyl]methanesulfonamideKi1.8 [1], 2.4 [2], 6.3 [3]
5-(3,5-Dimethyl-1,2-oxazol-4-yl)-1-[(3-fluorophenyl)methyl]pyridin-2-oneIC5030.0 [1], 1070.0 [2], 1410.0 [3]
2(1H)-Pyridinone, 5-(3,5-dimethyl-4-isoxazolyl)-1-(phenylmethyl)-IC5080.0 [1], 230.0 [2], 280.0 [3]
3-[2-(2,4-Difluorophenoxy)-5-methylsulfonylphenyl]-1-methyl-6H-pyrrolo[2,3-c]pyridin-7-oneKi77.0 [1], 98.0 [2], 280.0 [3]
N-[4-(2,2-Dimethylpropoxy)-3-(6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl]ethanesulfonamideKi13.6 [1], 17.8 [2], 38.0 [3]
N-[3-(6-Methyl-7-oxo-1H-pyrrolo[2,3-c]pyridin-4-yl)-4-pyrimidin-5-yloxyphenyl]ethanesulfonamideKi5.4 [1], 15.2 [2], 32.0 [3]
4-[2-(2,2-Difluorocyclopropyl)-7-(3,5-dimethyl-1H-pyrazol-4-yl)-3H-benzimidazol-5-yl]-3,5-dimethyl-1,2-oxazoleIC5025.1 [1], 94.1 [2], 160.5 [3]
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References

This online tool may be cited as follows

MLA

"Quest Database™ Bromodomain-containing protein 4 Inhibitors (IC50, Ki)." AAT Bioquest, Inc., 9 May. 2024, https://www.aatbio.com/data-sets/bromodomain-containing-protein-4-inhibitors-ic50-ki.

APA

AAT Bioquest, Inc. (2024, May 9). Quest Database™ Bromodomain-containing protein 4 Inhibitors (IC50, Ki). AAT Bioquest. https://www.aatbio.com/data-sets/bromodomain-containing-protein-4-inhibitors-ic50-ki.
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