 | 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 | 103.0 [1], 183.0 [2], 217.0 [3] |
 | 4-[(2s,4r)-1-Acetyl-4-[(4-Chlorophenyl)amino]-2-Methyl-1,2,3,4-Tetrahydroquinolin-6-Yl]benzoic Acid | IC50 | 50.12 [1], 31622.78 [2] |
 | BET Inhibitor C3 | IC50 | 2300.0 [1], 5200.0 [2] |
 | BET Inhibitor C3 | Ki | 450.0 [1] |
 | BI-2536 | IC50 | 260.0 [1], 1400.0 [2] |
 | Apabetalone | IC50 | 708.0 [1], 4836.0 [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 | 110.0 [1], 169.0 [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], 50118.72 [2] |
 | 5-(5-Methoxypyridin-3-Yl)-3-Methyl-8-[(Piperidin-4-Yl)amino]-1,2-Dihydro-1,7-Naphthyridin-2-One | IC50 | 6309.57 [1], 25118.86 [2] |
 | 3-Methyl-5-(5-methylpyridin-3-yl)-8-(piperidin-4-ylamino)-1H-1,7-naphthyridin-2-one | IC50 | 7943.28 [1], 31622.78 [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] |
 | 4-[(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-N-cyclopentylbenzenesulfonamide | IC50 | 3082.0 [1], 3292.0 [2] |
 | 6-[(2-Amino-4-hydroxy-5-methylphenyl)diazenyl]-3,4-dihydro-1H-quinolin-2-one | IC50 | 2781.0 [1], 3183.0 [2] |
 | 5-[(2S)-1-Acetyl-2-cyclopropyl-4-[[2-(hydroxymethyl)phenyl]methyl]-2,3-dihydroquinoxalin-6-yl]pyrimidine-2-carboxamide | IC50 | 100.0 [1], 501.19 [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 | 199.53 [1], 1584.89 [2] |
 | 8-(4-Methylphenyl)-13-(2,2,2-trifluoroethyl)-5-oxa-2,11,13-triazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | Ki | 450.0 [1], 850.0 [2] |
 | 4-(4-Fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)-1H-imidazole | IC50 | 20000.0 [1] |
 | 4-[[(7S)-8-Cyclopentyl-7-ethyl-5-methyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide | IC50 | 3513.0 [1] |
 | Dinaciclib | IC50 | 37000.0 [1] |
 | Fedratinib | IC50 | 340.0 [1] |
 | 8-(4-Dibenzothienyl)-2-(4-morpholinyl)-4H-1-benzopyran-4-one | IC50 | 3500.0 [1] |
 | CID 16722832 | IC50 | 230.0 [1] |
 | Mivebresib | Ki | 2.2 [1] |
 | 5-Ethyl-5-methyl-5,6-dihydrobenzo[h]quinazolin-4(3H)-one | IC50 | 220000.0 [1] |
 | 4-[(8-Cyclopentyl-5-methyl-6-oxo-7H-pteridin-2-yl)amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide | IC50 | 25990.0 [1] |
 | 11,13-Dimethyl-8-(4-methylphenyl)-5-oxa-2,11,13-triazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | Ki | 40000.0 [1] |
 | N-[3-(3-Methyl-4-Oxo-4,5,6,7-Tetrahydro-2h-Isoindol-1-Yl)-4-Phenoxyphenyl]methanesulfonamide | Ki | 110.0 [1] |
 | 1-[2-(2,4-Difluorophenoxy)-5-methylsulfonylphenyl]-3-methyl-2,5,6,7-tetrahydropyrrolo[3,4-c]pyridin-4-one | Ki | 140.0 [1] |
 | 3-[(4-Chlorophenyl)methyl]-7-Ethyl-Purine-2,6-Dione | IC50 | 2300.0 [1] |
 | 4-[[(7R)-8-Cyclopentyl-5,7-dimethyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide | IC50 | 342.0 [1] |
 | 4-[[(7R)-8-Cyclopentyl-5,7-dimethyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-piperidin-4-ylbenzamide | IC50 | 560.0 [1] |
 | 3-Butyl-7-ethylpurine-2,6-dione | IC50 | 7900.0 [1] |
 | 8-[(5-Amino-1H-1,2,4-triazol-3-yl)sulfanylmethyl]-3-[(4-chlorophenyl)methyl]-7-ethylpurine-2,6-dione | IC50 | 100000.0 [1] |
 | 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 | 100000.0 [1] |
 | 13-Cyclopropyl-8-(4-methylphenyl)-5-oxa-2,11,13-triazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | Ki | 40000.0 [1] |
 | 5-Benzyl-13-ethyl-8-(4-methylphenyl)-2,5,11,13-tetrazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | IC50 | 550.0 [1] |
 | 13-Ethyl-8-(4-methylphenyl)-5-oxa-2,11,13-triazatricyclo[7.4.0.03,7]trideca-1,3(7),8-triene-6,10,12-trione | Ki | 40000.0 [1] |
 | 4-(2,5-Dimethoxyphenyl)-3-methyl-5-propyl-2,4-dihydropyrrolo[3,4-c]pyrrol-6-one | IC50 | 67000.0 [1] |
 | 13-Ethyl-5-methyl-8-(4-methylphenyl)-2,5,11,13-tetrazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | Ki | 5600.0 [1] |
 | 8-(4-Methoxyphenyl)-13-methyl-5-oxa-2,11,13-triazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | Ki | 40000.0 [1] |
 | 13-Ethyl-11-methyl-8-(4-methylphenyl)-5-oxa-2,11,13-triazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | Ki | 40000.0 [1] |
 | 13-Ethyl-5-[2-(4-hydroxyphenyl)ethyl]-8-(4-methylphenyl)-2,5,11,13-tetrazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | IC50 | 760.0 [1] |
 | 13-Ethyl-8-(4-methylphenyl)-5-(2-phenylethyl)-2,5,11,13-tetrazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | IC50 | 1000.0 [1] |
 | 13-Ethyl-8-(4-methylphenyl)-2,11,13-triazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | Ki | 23000.0 [1] |
 | 13-Ethyl-8-[4-(trifluoromethyl)phenyl]-5-oxa-2,11,13-triazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | Ki | 4700.0 [1] |
 | 13-Ethyl-5-[2-(4-methoxyphenyl)ethyl]-8-(4-methylphenyl)-2,5,11,13-tetrazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | IC50 | 1000.0 [1] |
 | 8-(2-Hydroxyethylamino)-7-(naphthalen-1-ylmethyl)-3H-purine-2,6-dione | IC50 | 87000.0 [1] |
 | Methyl 4-[[(7R)-8-cyclopentyl-5,7-dimethyl-6-oxo-7H-pteridin-2-yl]amino]-3-cyclopentyloxybenzoate | IC50 | 933.0 [1] |
 | 4-[[(7R)-8-Cyclopentyl-5,7-dimethyl-6-oxo-7H-pteridin-2-yl]amino]-N-[2-(dimethylamino)ethyl]-3-methoxybenzamide | IC50 | 392.0 [1] |
 | N-Cyclohexyl-4-[[(7R)-8-cyclopentyl-5,7-dimethyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxybenzamide | IC50 | 378.0 [1] |
 | 4-[[(7R)-8-Cyclopentyl-5-methyl-6-oxo-7-propyl-7H-pteridin-2-yl]amino]-3-cyclopentyloxy-N-(1-methylpiperidin-4-yl)benzamide | IC50 | 1951.0 [1] |
 | 4-[[(7R)-5,7-Dimethyl-6-oxo-8-propan-2-yl-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide | IC50 | 978.0 [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-one | Ki | 5.9 [1] |
 | 4-[[(7R)-8-Cyclopentyl-5,7-dimethyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methyl-2H-pyridin-4-yl)benzamide | IC50 | 289.0 [1] |
 | 4-[[(7S)-8-Cyclopentyl-5,7-dimethyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide | IC50 | 229.0 [1] |
 | 4-[[(7R)-8-Cyclopentyl-5-methyl-6-oxo-7-propyl-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide | IC50 | 8468.0 [1] |
 | 3-Methoxy-4-[[(7R)-5-methyl-7-(2-methylpropyl)-8-(oxan-4-yl)-6-oxo-7H-pteridin-2-yl]amino]-N-(1-methylpiperidin-4-yl)benzamide | IC50 | 50000.0 [1] |
 | 4-[[(7R)-8-Cyclopentyl-5,7-dimethyl-6-oxo-7H-pteridin-2-yl]amino]-3-cyclopentyloxy-N-(1-methylpiperidin-4-yl)benzamide | IC50 | 102.0 [1] |
 | 4-[[(7R)-8-Cyclohexyl-5,7-dimethyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(1-methylpiperidin-4-yl)benzamide | IC50 | 750.0 [1] |
 | 4-[[(7S)-8-Cyclopentyl-5,7-dimethyl-6-oxo-7H-pteridin-2-yl]amino]-3-cyclopentyloxy-N-(1-methylpiperidin-4-yl)benzamide | IC50 | 245.0 [1] |
 | 4-[(8-Cyclopentyl-5-methyl-6-oxo-7H-pteridin-2-yl)amino]-3-cyclopentyloxy-N-(1-methylpiperidin-4-yl)benzamide | IC50 | 3543.0 [1] |
 | (7R)-8-Cyclopentyl-2-[2-methoxy-4-(piperidine-1-carbonyl)anilino]-5,7-dimethyl-7H-pteridin-6-one | IC50 | 369.0 [1] |
 | 4-[[(7R)-8-Cyclopentyl-5,7-dimethyl-6-oxo-7H-pteridin-2-yl]amino]-3-methoxy-N-(2-phenylethyl)benzamide | IC50 | 558.0 [1] |
 | 13-Methyl-8-phenyl-5-oxa-2,11,13-triazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | Ki | 40000.0 [1] |
 | 8-Phenyl-13-propyl-5-oxa-2,11,13-triazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | Ki | 2400.0 [1] |
 | 5-(2-Furyl)-1-(tetrahydro-2-furanylmethyl)pyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione | IC50 | 130000.0 [1] |
 | 8-Chloro-6-(4-chlorophenyl)-1-methyl-3H,4H-benzo[g]1,5-diazocin-2-one | IC50 | 220000.0 [1] |
 | 8-(4-Chlorophenyl)-13-ethyl-5-oxa-2,11,13-triazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | Ki | 1100.0 [1] |
 | 8-(4-Methoxyphenyl)-11,13-dimethyl-5-oxa-2,11,13-triazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | Ki | 40000.0 [1] |
 | 13-Ethyl-8-phenyl-5-oxa-2,11,13-triazatricyclo[7.4.0.03,7]trideca-1(9),3(7)-diene-6,10,12-trione | Ki | 1400.0 [1] |
 | 3-Butyl-8-[(6-butyl-5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)sulfanylmethyl]-7-ethylpurine-2,6-dione | IC50 | 100000.0 [1] |
 | 1,3-Diethyl-2-oxo-2,3-dihydro-1H-benzoimidazole-5-carbaldehyde | IC50 | 140000.0 [1] |
 | 7-(4-Fluorobenzyl)-3-methyl-8-(methylamino)-1H-purine-2,6(3H,7H)-dione | IC50 | 68000.0 [1] |
 | 3-[2-(2,4-Difluorophenoxy)-5-methylsulfonylphenyl]-1-methyl-6H-pyrrolo[2,3-c]pyridin-7-one | Ki | 490.0 [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-one | Ki | 0.69 [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-one | Ki | 4.2 [1] |
 | N-Methoxy-N'-(7-pyridin-3-yl-[1,2,4]triazolo[1,5-a]pyrimidin-2-yl)methanimidamide | IC50 | 120000.0 [1] |
 | 5-(3,5-Dimethyl-1,2-oxazol-4-yl)-3-hydroxy-3-(2-oxocyclohexyl)-1H-indol-2-one | IC50 | 58.0 [1] |
 | 5-(3,5-Dimethyl-1,2-oxazol-4-yl)-3-[[(2R)-1-hydroxypropan-2-yl]amino]-3-phenyl-1H-indol-2-one | IC50 | 69.0 [1] |
 | 3-Amino-5-(3,5-dimethyl-1,2-oxazol-4-yl)-3-phenyl-1H-indol-2-one | IC50 | 95.0 [1] |
 | 5-(3,5-Dimethyl-1,2-oxazol-4-yl)-3-[(3S)-3-hydroxypiperidin-1-yl]-3-phenyl-1H-indol-2-one | IC50 | 23.0 [1] |
 | 3-Cyclohexyl-5-(3,5-dimethyl-1,2-oxazol-4-yl)-3-[[(2R)-2-hydroxypropyl]amino]-1H-indol-2-one | IC50 | 42.0 [1] |
 | 3-[(3S)-3-Aminopiperidin-1-yl]-5-(3,5-dimethyl-1,2-oxazol-4-yl)-3-phenyl-1H-indol-2-one | IC50 | 14.0 [1] |
 | 5-(3,5-Dimethyl-1,2-oxazol-4-yl)-3-hydroxy-3-thiophen-3-yl-1H-indol-2-one | IC50 | 31.0 [1] |
 | 5-(3,5-Dimethyl-1,2-oxazol-4-yl)-3-hydroxy-3-(oxan-4-yl)-1H-indol-2-one | IC50 | 510.0 [1] |