 | 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]acetate | IC50 | 53.3 [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]acetate | Ki | 12.5 [1], 13.2 [2] |
 | Molibresib | IC50 | 32.5 [1], 150.0 [2], 790.0 [3], 810.0 [4] |
| Molibresib | Ki | 49.2 [1], 56.8 [2] |
 | Birabresib | IC50 | 24.8 [1], 33.3 [2], 92.0 [3] |
| Birabresib | Ki | 5.4 [1], 16.6 [2] |
 | 4-[(2s,4r)-1-Acetyl-4-[(4-Chlorophenyl)amino]-2-Methyl-1,2,3,4-Tetrahydroquinolin-6-Yl]benzoic Acid | IC50 | 3.16 [1], 30.0 [2], 158.49 [3], 720.0 [4], 31622.78 [5] |
 | I-Bet151 (gsk1210151A) | IC50 | 500.0 [1], 501.19 [2] |
| I-Bet151 (gsk1210151A) | Ki | 9.0 [1], 49.6 [2] |
 | 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]acetate | IC50 | 16.0 [1], 17.0 [2], 26.1 [3], 144.0 [4] |
 | Benzyl [(4r)-1-Methyl-6-Phenyl-4h-[1,2,4]triazolo[4,3-A][1,4]benzodiazepin-4-Yl]carbamate | IC50 | 29.9 [1], 160.0 [2], 820.0 [3] |
 | Apabetalone | IC50 | 251.0 [1], 5780.0 [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-one | IC50 | 31622.78 [1] |
 | 1-[1-(Pyridin-2-Yl)indolizin-3-Yl]ethan-1-One | IC50 | 2000.0 [1], 12600.0 [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-oxazole | Ki | 11.1 [1], 11.7 [2] |
 | 5-(5-Methoxypyridin-3-Yl)-3-Methyl-8-[(Piperidin-4-Yl)amino]-1,2-Dihydro-1,7-Naphthyridin-2-One | IC50 | 3981.07 [1], 19952.62 [2] |
 | 3-Methyl-5-(5-methylpyridin-3-yl)-8-(piperidin-4-ylamino)-1H-1,7-naphthyridin-2-one | IC50 | 6309.57 [1], 19952.62 [2] |
 | 3-[(4-Chlorophenyl)methyl]-7-Ethyl-Purine-2,6-Dione | IC50 | 1600.0 [1], 4700.0 [2] |
 | 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-oxazole | Ki | 12.2 [1], 22.2 [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-one | IC50 | 50118.72 [1] |
 | Propan-2-yl N-[(2S,4R)-1-acetyl-6-(furan-2-yl)-2-methyl-3,4-dihydro-2H-quinolin-4-yl]carbamate | IC50 | 610.0 [1], 2020.0 [2] |
 | 7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 43.0 [1], 129.0 [2] |
 | Methyl 7-(4-chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxylate | IC50 | 52.0 [1], 116.0 [2] |
 | 7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxylic acid | IC50 | 50.0 [1], 185.0 [2] |
 | 7-Benzyl-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 999.0 [1] |
 | 7-(4-Chlorophenyl)-1-methyl-9-(2H-tetrazol-5-yl)-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 6.0 [1], 7.0 [2] |
 | 7-(4-Chlorophenyl)-1-methyl-9-(1H-pyrazol-5-yl)-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 25.0 [1], 35.0 [2] |
 | 5-[7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepin-9-yl]pyrimidin-2-amine | IC50 | 38.0 [1], 64.0 [2] |
 | (5S)-7-(4-Chlorophenyl)-1,5-dimethyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 34.0 [1], 53.0 [2] |
 | (5R)-7-(4-Chlorophenyl)-1,5-dimethyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 25.0 [1], 38.0 [2] |
 | N-Benzhydryl-7-(4-chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 44.0 [1], 151.0 [2] |
 | 7-(4-Chlorophenyl)-N-[(1S)-1-(4-fluorophenyl)ethyl]-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 4.0 [1], 95.0 [2] |
 | 2-[7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepin-5-yl]ethanol | IC50 | 45.0 [1], 340.0 [2] |
 | [7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepin-9-yl]methanol | IC50 | 40.0 [1], 388.0 [2] |
 | 7-(4-Chlorophenyl)-1-methyl-9-(6-methylpyridin-3-yl)-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 28.0 [1], 53.0 [2] |
 | 7-(4-Chlorophenyl)-1-methyl-N-methylsulfonyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 25.0 [1], 44.0 [2] |
 | 1-Methyl-7-phenyl-5H-triazolo[1,5-d][1,4]benzodiazepin-6-one | IC50 | 10000.0 [1] |
 | 5-[7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepin-9-yl]pyridin-2-amine | IC50 | 21.0 [1], 33.0 [2] |
 | 1-Methyl-7-phenyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 39.0 [1], 263.5 [2] |
 | N-(Benzenesulfonyl)-7-(4-chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 25.0 [1], 54.0 [2] |
 | 7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 17.0 [1], 34.0 [2] |
 | 7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carbonitrile | IC50 | 24.0 [1], 56.0 [2] |
 | 1-[7-(4-Chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepin-9-yl]-2,2,2-trifluoroethanol | IC50 | 204.0 [1], 370.0 [2] |
 | 7-(4-Chlorophenyl)-1-methyl-N-phenyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 18.0 [1], 79.0 [2] |
 | N-Benzyl-7-(4-chlorophenyl)-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 37.0 [1], 136.0 [2] |
 | 7-(4-Chlorophenyl)-1-methyl-N-[(1S)-1-phenylethyl]-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 3.0 [1], 51.0 [2] |
 | 7-(4-Chlorophenyl)-1-methyl-N-[(1R)-1-phenylethyl]-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine-9-carboxamide | IC50 | 20.0 [1], 68.0 [2] |
 | 3-Butyl-7-ethylpurine-2,6-dione | IC50 | 6600.0 [1], 18800.0 [2] |
 | Propan-2-yl N-[(2S,4R)-1-acetyl-2-methyl-6-thiophen-2-yl-3,4-dihydro-2H-quinolin-4-yl]carbamate | IC50 | 830.0 [1], 1770.0 [2] |
 | Propan-2-yl N-[(2S,4R)-1-acetyl-2-methyl-6-(1H-pyrrol-3-yl)-3,4-dihydro-2H-quinolin-4-yl]carbamate | IC50 | 410.0 [1], 2480.0 [2] |
 | Propan-2-yl N-[(2S,4R)-1-acetyl-6-(furan-3-yl)-2-methyl-3,4-dihydro-2H-quinolin-4-yl]carbamate | IC50 | 1910.0 [1], 5800.0 [2] |
 | Propan-2-yl N-[(2S,4R)-1-acetyl-2-methyl-6-(1H-pyrrol-2-yl)-3,4-dihydro-2H-quinolin-4-yl]carbamate | IC50 | 1400.0 [1] |
 | Propan-2-yl N-[(2S,4R)-1-acetyl-2-methyl-6-thiophen-3-yl-3,4-dihydro-2H-quinolin-4-yl]carbamate | IC50 | 1080.0 [1], 5210.0 [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-carboxamide | IC50 | 3.1 [1], 3.9 [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-one | IC50 | 24600.0 [1], 100000.0 [2] |
 | 4-[(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-cyclopentylbenzenesulfonamide | IC50 | 772.0 [1], 1836.0 [2] |
 | 6-[(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-3,4-dihydro-1H-quinolin-2-one | IC50 | 803.0 [1], 1736.0 [2] |
 | 5-[(2S)-1-Acetyl-2-cyclopropyl-4-[[2-(hydroxymethyl)phenyl]methyl]-2,3-dihydroquinoxalin-6-yl]pyrimidine-2-carboxamide | IC50 | 100.0 [1], 1584.89 [2] |
 | 1-[(2S)-2-Cyclopropyl-4-[[2-(hydroxymethyl)phenyl]methyl]-6-(1,2,3,6-tetrahydropyridin-4-yl)-2,3-dihydroquinoxalin-1-yl]ethanone | IC50 | 316.23 [1], 2511.89 [2] |
 | 7-(4-Chlorophenyl)-1-methyl-9-(pyrazol-1-ylmethyl)-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 147.0 [1], 273.0 [2] |
 | 7-[(3-Bromophenyl)methyl]-1-methyl-5,6-dihydrotriazolo[1,5-d][1,4]benzodiazepine | IC50 | 44.0 [1], 129.0 [2] |
 | 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-6-methoxy-N-methyl-9H-pyrimido[4,5-b]indole-2-carboxamide | IC50 | 218.0 [1], 224.0 [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-oxazole | Ki | 15.4 [1], 21.0 [2] |
 | 2-(4-Morpholinyl)-8-phenyl-4H-1-benzopyran-4-one | IC50 | 10300.0 [1] |
 | 2-Piperazinyl-8-phenyl-4H-1-benzopyran-4-one | IC50 | 7400.0 [1] |
 | Mivebresib | Ki | 1.0 [1] |
 | 4-[4-[(Dimethylamino)methyl]-2,5-Dimethoxy-Phenyl]-2-Methyl-2,7-Naphthyridin-1-One | IC50 | 100000.0 [1] |
 | 1-[2-(1H-Benzimidazol-2-ylsulfanyl)ethyl]-3-methyl-1,3-dihydro-2H-benzimidazole-2-thione | IC50 | 28000.0 [1] |
 | 3,5 Dimethyl-4-Phenyl-1,2-Oxazole | IC50 | 34300.0 [1] |
 | 4-[4-[(Dimethylamino)methyl]-3,5-Dimethoxy-Phenyl]-2-Methyl-2,7-Naphthyridin-1-One | IC50 | 100000.0 [1] |
 | Benzyl N-(1-methyl-6-phenyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl)carbamate | IC50 | 1258.93 [1] |
 | 1-[3-(3,5-Dimethyl-1,2-oxazol-4-yl)-5-ethoxyphenyl]ethanol | IC50 | 1600.0 [1] |
 | 4-[(2-Tert-Butylphenyl)amino]-7-(3,5-Dimethyl-1,2-Oxazol-4-Yl)quinoline-3-Carboxylic Acid | IC50 | 794.33 [1] |
 | 5-{4-[(Dimethylamino)methyl]-3,5-dimethoxyphenyl}-1,3,6-trimethyl-1,2-dihydro-pyridin-2-one | IC50 | 33234.0 [1] |
 | 4-{4-[(Dimethylamino)methyl]-3,5-dimethoxyphenyl}-2-methyl-1,2-dihydroisoquinolin-1-one | IC50 | 50857.0 [1] |
 | 5-(2-Amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-tert-butylpyridine-3-sulfonamide | IC50 | 10000.0 [1] |
 | 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-(pyridin-2-ylmethyl)-3H-imidazo[4,5-c]quinolin-2-one | IC50 | 1584.89 [1] |
 | 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-[(1R)-1-phenylethyl]-3H-imidazo[4,5-c]quinolin-2-one | IC50 | 398.11 [1] |
 | 3-(3,5-Dimethyl-1,2-Oxazol-4-Yl)-5-Ethoxybenzoic Acid | IC50 | 28200.0 [1] |
 | 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-1-(2-fluorophenyl)-8-methoxy-3H-imidazo[4,5-c]quinolin-2-one | IC50 | 2511.89 [1] |
 | 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-8-methoxy-1-[(1S)-1-phenylethyl]-3H-imidazo[4,5-c]quinolin-2-one | IC50 | 1995.26 [1] |
 | 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-4-(2-fluoroanilino)quinoline-3-carboxamide | IC50 | 12589.25 [1] |
 | 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-4-(2-fluoroanilino)-6-methoxyquinoline-3-carboxamide | IC50 | 501.19 [1] |
 | 7-(3,5-Dimethyl-1,2-oxazol-4-yl)-6-methoxy-4-(quinolin-8-ylamino)quinoline-3-carboxamide | IC50 | 1000.0 [1] |
 | 1-(2-Tert-butylphenyl)-7-(3,5-dimethyl-1,2-oxazol-4-yl)-8-methoxy-3H-imidazo[4,5-c]quinolin-2-one | IC50 | 501.19 [1] |
 | 4-(Cyclohexylamino)-7-(3,5-dimethyl-1,2-oxazol-4-yl)-6-methoxyquinoline-3-carboxamide | IC50 | 1995.26 [1] |
 | 1-Benzyl-7-(3,5-dimethyl-1,2-oxazol-4-yl)-8-methoxy-3H-imidazo[4,5-c]quinolin-2-one | IC50 | 501.19 [1] |
 | N-[3-(3-Methyl-4-Oxo-4,5,6,7-Tetrahydro-2h-Isoindol-1-Yl)-4-Phenoxyphenyl]methanesulfonamide | Ki | 14.0 [1] |
 | 1-[2-(2,4-Difluorophenoxy)-5-methylsulfonylphenyl]-3-methyl-2,5,6,7-tetrahydropyrrolo[3,4-c]pyridin-4-one | Ki | 27.0 [1] |
 | 4-[(5-Phenylpyridin-3-Yl)carbonyl]-3,4-Dihydroquinoxalin-2(1h)-One | IC50 | 20000.0 [1] |
 | 1-[(2S,4R)-4-Anilino-2-methyl-6-phenyl-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 794.33 [1] |
 | 4-[(2S,4R)-1-Acetyl-4-anilino-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzonitrile | IC50 | 1000.0 [1] |
 | 1-[(2S,4R)-4-Anilino-2-methyl-6-[4-(trifluoromethyl)phenyl]-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 1995.26 [1] |
 | 1-[(2S,4R)-4-Anilino-6-(4-methoxyphenyl)-2-methyl-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 1258.93 [1] |
 | 1-[(2S,4R)-4-Anilino-6-[4-(hydroxymethyl)phenyl]-2-methyl-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 794.33 [1] |
 | 1-[(2S,4R)-4-Anilino-2-methyl-6-[4-(morpholin-4-ylmethyl)phenyl]-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 794.33 [1] |
 | 1-[(2S,4R)-4-Anilino-2-methyl-6-[3-(piperidin-1-ylmethyl)phenyl]-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 1258.93 [1] |
 | 1-[(2R,4S)-4-Anilino-2-methyl-6-[4-(piperidin-1-ylmethyl)phenyl]-3,4-dihydro-2H-quinolin-1-yl]ethanone | IC50 | 25118.86 [1] |
 | Methyl 4-[(2S,4R)-1-acetyl-4-(4-tert-butylanilino)-2-methyl-3,4-dihydro-2H-quinolin-6-yl]benzoate | IC50 | 501.19 [1] |
 | 4-[(2S,4R)-1-Acetyl-2-methyl-4-(4-methylsulfonylanilino)-3,4-dihydro-2H-quinolin-6-yl]benzoic acid | IC50 | 1000.0 [1] |
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