| Palbociclib | IC50 | 16.0 [1], 21.0 [2] |
| Abemaciclib | IC50 | 1.9 [1], 7.8 [2], 10.0 [3] |
| Quercetin | IC50 | 25000.0 [1] |
| Apigenin | IC50 | 1700.0 [1] |
| Kaempferol | IC50 | 22000.0 [1] |
| Luteolin | IC50 | 300000.0 [1] |
| Alvocidib | IC50 | 80.0 [1] |
| Chrysin | IC50 | 6000.0 [1] |
| Fisetin | IC50 | 850.0 [1] |
| Ribociclib | IC50 | 6.0 [1], 39.0 [2] |
| (13R,15S)-13-Methyl-16-oxa-8,9,12,22,24-pentazahexacyclo[15.6.2.16,9.112,15.02,7.021,25]heptacosa-1(24),2,4,6,17,19,21(25)-heptaene-23,27-dione | IC50 | 12.0 [1] |
| Fascaplysin | IC50 | 3400.0 [1] |
| Sulfuretin | IC50 | 2440.0 [1] |
| 4-[[6-(Ethylamino)-2-[[1-(phenylmethyl)-5-indolyl]amino]-4-pyrimidinyl]amino]-1-cyclohexanol | IC50 | 5600.0 [1] |
| N'-(Pyrrolidino[2,1-B]isoindolin-4-ON-8-YL)-N-(pyridin-2-YL)urea | IC50 | 71.0 [1] |
| 7-Chloro-3-oxo-8-(1,3-thiazol-5-ylmethylamino)-11,16-dioxa-2,4,19,21-tetrazatricyclo[15.3.1.05,10]henicosa-1(20),5,7,9,17(21),18-hexaene-18-carbonitrile | Ki | 1549.0 [1] |
| 5-(2-Amino-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-N-tert-butylpyridine-3-sulfonamide | IC50 | 10000.0 [1] |
| 2-Bromo-N-(2,5-dichlorothiophen-3-yl)sulfonyl-N-phenylacetamide | IC50 | 20000.0 [1] |
| N-[4-[(4-Methylpiperazin-1-yl)methyl]phenyl]-4-(thieno[2,3-d]pyrimidin-4-ylamino)-1H-pyrazole-5-carboxamide | IC50 | 3.33 [1] |
| N-[5-[(4-Ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine | IC50 | 0.9 [1] |
| 5-Fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-[(4-methylpiperazin-1-yl)methyl]pyridin-2-yl]pyrimidin-2-amine | IC50 | 4.0 [1] |
| 5-Fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-(piperazin-1-ylmethyl)pyridin-2-yl]pyrimidin-2-amine | IC50 | 3.7 [1] |
| N-[5-[(4-Ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(5-fluoro-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine | IC50 | 244.1 [1] |
| 6-(7-Fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)-N-[5-[(4-propan-2-ylpiperazin-1-yl)methyl]pyrazin-2-yl]pyrimidin-4-amine | IC50 | 2.3 [1] |
| N-[5-[(1-Ethylpiperidin-4-yl)methyl]pyrazin-2-yl]-6-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-4-amine | IC50 | 2.9 [1] |
| 5-[(4-Ethylpiperazin-1-yl)methyl]-N-[4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyridin-2-yl]pyridin-2-amine | IC50 | 2.9 [1] |
| 5-[(4-Ethylpiperazin-1-yl)methyl]-N-[4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyridin-2-yl]pyrazin-2-amine | IC50 | 1.6 [1] |
| 6-[(4-Ethylpiperazin-1-yl)methyl]-N-[4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyridin-2-yl]pyridazin-3-amine | IC50 | 23.6 [1] |
| N-[5-[(4-Ethylpiperazin-1-yl)methyl]pyrazin-2-yl]-6-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-4-amine | IC50 | 2.7 [1] |
| 6-(7-Fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)-N-[5-[[4-(2,2,2-trifluoroethyl)piperazin-1-yl]methyl]pyrazin-2-yl]pyrimidin-4-amine | IC50 | 5.8 [1] |
| N-[5-[(4-Cyclopentylpiperazin-1-yl)methyl]pyrazin-2-yl]-6-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-4-amine | IC50 | 1.8 [1] |
| 6-(7-Fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)-N-[5-[[4-(2-methoxyethyl)piperazin-1-yl]methyl]pyrazin-2-yl]pyrimidin-4-amine | IC50 | 1.6 [1] |
| N-[5-[[4-(Cyclopropylmethyl)piperazin-1-yl]methyl]pyrazin-2-yl]-6-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-4-amine | IC50 | 2.2 [1] |
| 5-[(4-Ethylpiperazin-1-yl)methyl]-N-[5-fluoro-4-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyridin-2-yl]pyrazin-2-amine | IC50 | 1.6 [1] |
| N-[5-[(4-Ethylpiperazin-1-yl)methyl]pyridin-2-yl]-6-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-4-amine | IC50 | 4.4 [1] |
| N-[5-(1-Ethylpiperidin-4-yl)oxypyrazin-2-yl]-6-(7-fluoro-2-methyl-3-propan-2-ylbenzimidazol-5-yl)pyrimidin-4-amine | IC50 | 4.0 [1] |
| N-[5-[(4-Ethylpiperazin-1-yl)methyl]-6-methylpyridin-2-yl]-5-fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine | IC50 | 46.0 [1] |
| N-[5-[(4-Ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(5-fluoro-2,2-dimethyl-1,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine | IC50 | 36.0 [1] |
| 5-Fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-[[4-(2-fluoroethyl)piperazin-1-yl]methyl]pyridin-2-yl]pyrimidin-2-amine | IC50 | 11.2 [1] |
| 5-Fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)-N-[6-methyl-5-[(4-methylpiperazin-1-yl)methyl]pyridin-2-yl]pyrimidin-2-amine | IC50 | 271.0 [1] |
| N-[5-[(4-Cyclopropylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine | IC50 | 19.0 [1] |
| 4-(2-Ethyl-5-fluoro-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoropyrimidin-2-amine | IC50 | 339.0 [1] |
| 5-Fluoro-4-(5-fluoro-1-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-[(4-propan-2-ylpiperazin-1-yl)methyl]pyridin-2-yl]pyrimidin-2-amine | IC50 | 12.7 [1] |
| 4-(1-Ethyl-5-fluoro-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoropyrimidin-2-amine | IC50 | 22.0 [1] |
| N-[5-[(4-Ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(5-fluoro-1-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine | IC50 | 28.0 [1] |
| N-[5-[(4-Ethylpiperazin-1-yl)methyl]-6-methylpyridin-2-yl]-5-fluoro-4-(5-fluoro-1-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine | IC50 | 178.0 [1] |
| 5-Fluoro-4-(5-fluoro-1-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-[(4-methylpiperazin-1-yl)methyl]pyridin-2-yl]pyrimidin-2-amine | IC50 | 275.0 [1] |
| N-[5-[(4-Ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(5-fluoro-2-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine | IC50 | 392.0 [1] |
| 4-(1-Ethyl-5-fluoro-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)-5-fluoro-N-[5-[(4-methylpiperazin-1-yl)methyl]pyridin-2-yl]pyrimidin-2-amine | IC50 | 2.4 [1] |
| N-[5-[(4-Ethylpiperazin-1-yl)methyl]pyridin-2-yl]-4-(5-fluoro-1-methyl-2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine | IC50 | 752.0 [1] |
| N-[5-[(4-Ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(4-fluoro-7,8,9,10-tetrahydro-6H-azepino[1,2-a]benzimidazol-2-yl)pyrimidin-2-amine | IC50 | 247.8 [1] |
| N-[5-[(4-Ethylpiperazin-1-yl)methyl]pyridin-2-yl]-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)pyrimidin-2-amine | IC50 | 17.4 [1] |
| N-[5-[(4-Ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoro-4-(6-fluoro-1,2,3,4-tetrahydropyrido[1,2-a]benzimidazol-8-yl)pyrimidin-2-amine | IC50 | 45.6 [1] |
| 4-(1,1-Dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)-N-[5-[(4-ethylpiperazin-1-yl)methyl]pyridin-2-yl]-5-fluoropyrimidin-2-amine | IC50 | 15.8 [1] |
| 5-Fluoro-4-(5-fluoro-1,1-dimethyl-2,3-dihydropyrrolo[1,2-a]benzimidazol-7-yl)-N-[6-methyl-5-(piperazin-1-ylmethyl)pyridin-2-yl]pyrimidin-2-amine | IC50 | 18.7 [1] |
| Clk1-IN-1 | IC50 | 10000.0 [1] |
| 6-Acetyl-8-cyclopentyl-2-[[5-[4-[2-(3-methoxypropylamino)acetyl]piperazin-1-yl]pyridin-2-yl]amino]-5-methylpyrido[2,3-d]pyrimidin-7-one | IC50 | 18.0 [1] |
| 6-Acetyl-8-cyclopentyl-2-[[5-(4-ethylpiperazin-1-yl)pyridin-2-yl]amino]-5-methylpyrido[2,3-d]pyrimidin-7-one | IC50 | 34.0 [1] |
| Acetyloxymethyl 4-[6-[(6-acetyl-8-cyclopentyl-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]pyridin-3-yl]piperazine-1-carboxylate | IC50 | 28.0 [1] |
| 6-Acetyl-2-[[5-[4-[2-(2-aminoethylamino)acetyl]piperazin-1-yl]pyridin-2-yl]amino]-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidin-7-one | IC50 | 23.0 [1] |
| 4-Chloro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-isoquinolin-6-ylpyridin-2-yl]phenol | IC50 | 1000.0 [1] |
| 4-Fluoro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol | IC50 | 1000.0 [1] |
| 5-Fluoro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol | IC50 | 1000.0 [1] |
| 4-Chloro-2-[5-[[(1R)-2-hydroxy-1-phenylethyl]amino]-3-(3-methyl-2H-indazol-5-yl)pyridin-2-yl]phenol | IC50 | 1000.0 [1] |
| 4-[(2-Methyl-6-propan-2-ylthieno[2,3-d]pyrimidin-4-yl)amino]-N-[4-(morpholin-4-ylmethyl)phenyl]-1H-pyrazole-5-carboxamide | IC50 | 33.21 [1] |
| N-[4-[(4-Methylpiperazin-1-yl)methyl]phenyl]-4-[(2-methyl-6-propan-2-ylthieno[2,3-d]pyrimidin-4-yl)amino]-1H-pyrazole-5-carboxamide | IC50 | 19.24 [1] |
| 4-[(2-Methylthieno[2,3-d]pyrimidin-4-yl)amino]-N-(4-piperazin-1-ylphenyl)-1H-pyrazole-5-carboxamide | IC50 | 84.31 [1] |
| N-[2-(Dimethylamino)ethyl]-N-methyl-4-[(8-methylsulfanyl-5,6-dihydropyrimido[4,5-f]quinazolin-2-yl)amino]benzamide | IC50 | 5000.0 [1] |
| 5-(2-Cyclohexyloxy-6-methylpyrimidin-4-yl)-N-[5-[(4-methylpiperazin-1-yl)methyl]pyrazin-2-yl]-1,3-thiazol-2-amine | IC50 | 7.8 [1] |
| 4-(2-Chloro-4-fluorophenyl)-8-(2,6-dichlorophenyl)-7-oxido-1,7-naphthyridin-7-ium | IC50 | 10000.0 [1] |
| 9-Cyclopentyl-N-(5-Piperazin-1-Ylpyridin-2-Yl)pyrido[4,5]pyrrolo[1,2-D]pyrimidin-2-Amine | IC50 | 4.4 [1] |
| 8-Cyclopentyl-5-[(5-piperazin-1-ylpyridin-2-yl)amino]-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaene-10-carbonitrile | IC50 | 13.4 [1] |
| 10-Chloro-8-cyclopentyl-N-(5-piperazin-1-ylpyridin-2-yl)-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine | IC50 | 4.3 [1] |
| 8-(4-Methylcyclohexyl)-N-(5-piperazin-1-ylpyridin-2-yl)-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine | IC50 | 4.4 [1] |
| 8-Cyclopentyl-5-[(5-piperazin-1-ylpyridin-2-yl)amino]-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,12-pentaen-10-one | IC50 | 11.0 [1] |
| 8-Cyclopentyl-10-fluoro-N-(5-piperazin-1-ylpyridin-2-yl)-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine | IC50 | 17.0 [1] |
| 8-Cyclohexyl-N-(5-piperazin-1-ylpyridin-2-yl)-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine | IC50 | 13.1 [1] |
| 8-(4,4-Dimethylcyclohexyl)-N-(5-piperazin-1-ylpyridin-2-yl)-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine | IC50 | 1.1 [1] |
| (2S)-2-[5-[(5-Piperazin-1-ylpyridin-2-yl)amino]-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-8-yl]propan-1-ol | IC50 | 29.0 [1] |
| 8-Cyclopentyl-N-(5-piperazin-1-ylpyridin-2-yl)-4,6,8,10,11-pentazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine | IC50 | 13.0 [1] |
| 8-Cyclopentyl-10-methyl-N-(5-piperazin-1-ylpyridin-2-yl)-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine | IC50 | 47.0 [1] |
| 4-[5-[(5-Piperazin-1-ylpyridin-2-yl)amino]-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-8-yl]cyclohexan-1-ol | IC50 | 5.9 [1] |
| (3R)-1-[2-[4-(4-Acetylphenyl)piperazin-1-yl]-2-oxoethyl]-N-(3-chloro-4-hydroxyphenyl)pyrrolidine-3-carboxamide | IC50 | 50000.0 [1] |
| N-[(4-Methoxyphenyl)carbamothioyl]-1,3-diphenylpyrazole-4-carboxamide | IC50 | 50.0 [1] |
| N-[(4-Methoxyphenyl)carbamothioyl]-3-(4-methylphenyl)-1-phenylpyrazole-4-carboxamide | IC50 | 43.0 [1] |
| 3-(4-Chlorophenyl)-N-[(4-methoxyphenyl)carbamothioyl]-1-phenylpyrazole-4-carboxamide | IC50 | 42.0 [1] |
| 3-(4-Fluorophenyl)-N-[(4-methoxyphenyl)carbamothioyl]-1-phenylpyrazole-4-carboxamide | IC50 | 33.0 [1] |
| 3-(4-Methoxyphenyl)-N-[(4-methoxyphenyl)carbamothioyl]-1-phenylpyrazole-4-carboxamide | IC50 | 29.0 [1] |
| (3S,4S)-3-Methoxy-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.12,6.07,28.08,13.015,19.020,27.021,26]nonacosa-8,10,12,14,19,21,23,25,27-nonaen-16-one | IC50 | 242.6 [1] |
| 8-Cyclopentyl-N-(2-piperazin-1-ylpyrimidin-5-yl)-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine | IC50 | 1.1 [1] |
| 9-Cycloheptyl-N-(5-piperazin-1-ylpyridin-2-yl)pyrimido[4,5-b]indol-2-amine | IC50 | 3.1 [1] |
| 3-N-(8-Cyclopentyl-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-yl)-6-N-[(3S)-pyrrolidin-3-yl]pyridazine-3,6-diamine | IC50 | 15.1 [1] |
| 8-Cyclopentyl-N-[5-[3-(trifluoromethyl)piperazin-1-yl]pyridin-2-yl]-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine | IC50 | 21.0 [1] |
| 8-Cyclopentyl-N-[5-(piperazin-1-ylmethyl)pyridin-2-yl]-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine | IC50 | 33.0 [1] |
| 8-Cyclopentyl-N-[6-(3,6-dihydro-2H-pyridin-1-yl)pyridazin-3-yl]-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine | IC50 | 40.0 [1] |
| (3R)-1-[6-[[8-[(2R)-Butan-2-yl]-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-yl]amino]pyridin-3-yl]pyrrolidin-3-ol | IC50 | 50.0 [1] |
| 8-(2-Methoxyethyl)-N-(6-piperazin-1-ylpyridazin-3-yl)-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine | IC50 | 400.0 [1] |
| N-(8-Cyclopentyl-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-yl)-4-(piperazin-1-ylmethyl)-1,3-thiazol-2-amine | IC50 | 6.2 [1] |
| 8-Cyclopentyl-11-methoxy-N-(5-piperazin-1-ylpyridin-2-yl)-4,6,8,10-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-5-amine | IC50 | 16.0 [1] |
| (2R)-1-[5-[[5-[4-(Dimethylamino)piperidin-1-yl]pyridin-2-yl]amino]-4,6,8,11-tetrazatricyclo[7.4.0.02,7]trideca-1(9),2,4,6,10,12-hexaen-8-yl]propan-2-ol | IC50 | 314.0 [1] |