| TTK | TTK | Other | 3h9f | A | B | 9-cyclopentyl-2-(4-(4-hydroxypiperidin-1-yl)-2-methoxyphenylamino)-5-methyl-8,9-dihydro-5h-pyrimido[4,5-b][1,4]diazepin-6(7h)-one | Human | 4712 | 0.49 | |
| PLK1 | PLK | Other | 4j52 | A | B | 4-{[(7r)-9-cyclopentyl-7-ethenyl-7-fluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5h-pyrimido[4,5-b][1,4]diazepin-2-yl]amino}-3-methoxy-n-(4-methylpiperazin-1-yl)benzamide | Human | 4976 | 0.53 | |
| PLK2 | PLK | Other | 4i6h | A | B | (7r)-8-cyclopentyl-7-ethyl-5-methyl-2-[2-(1,3-thiazol-4-yl)-1h-imidazol-1-yl]-7,8-dihydropteridin-6(5h)-one | Human | 5561 | 0.43 | |
| PLK2 | PLK | Other | 4i6b | A | A | (7r)-8-cyclopentyl-7-ethyl-5-methyl-7,8-dihydropteridin-6(5h)-one | Human | 5565 | 0.44 | |
| PLK2 | PLK | Other | 4i6b | A | B | (7r)-8-cyclopentyl-7-ethyl-5-methyl-7,8-dihydropteridin-6(5h)-one | Human | 5562 | 0.44 | |
| PLK2 | PLK | Other | 4i5p | A | A | (7r)-8-cyclopentyl-7-ethyl-5-methyl-2-(1h-pyrrol-2-yl)-7,8-dihydropteridin-6(5h)-one | Human | 5559 | 0.48 | |
| PLK2 | PLK | Other | 4i6h | A | A | (7r)-8-cyclopentyl-7-ethyl-5-methyl-2-[2-(1,3-thiazol-4-yl)-1h-imidazol-1-yl]-7,8-dihydropteridin-6(5h)-one | Human | 5558 | 0.43 | |
| PLK2 | PLK | Other | 4i6f | A | A | (7r)-8-cyclopentyl-7-ethyl-5-methyl-2-(2-phenyl-1h-imidazol-1-yl)-7,8-dihydropteridin-6(5h)-one | Human | 5564 | 0.45 | |
| PLK2 | PLK | Other | 4i5p | A | B | (7r)-8-cyclopentyl-7-ethyl-5-methyl-2-(1h-pyrrol-2-yl)-7,8-dihydropteridin-6(5h)-one | Human | 5560 | 0.48 | |
| CHEK1 (CHK1) | CAMKL | CAMK | 5oq6 | A | | 2-[(2-methoxy-4-{[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl}phenyl)amino]-5,11-dimethyl-5,11-dihydro-6h-pyrimido[4,5-b][1,4]benzodiazepin-6-one | Human | 8610 | 0.54 | |
| MAPK7 (Erk5) | MAPK | CMGC | 5byy | A | A | 2-{[2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl]amino}-5,11-dimethyl-5,11-dihydro-6h-pyrimido[4,5-b][1,4]benzodiazepin-6-one | Human | 6591 | 0.42 | |
| PLK1 | PLK | Other | 5ta6 | A | B | 4-{[(6r)-7-cyano-5-cyclopentyl-6-ethyl-5,6-dihydroimidazo[1,5-f]pteridin-3-yl]amino}-3-methoxy-n-(1-methylpiperidin-4-yl)benzamide | Human | 7462 | 0.73 | |
| FLT3 | PDGFR | TK | 6jqr | A | | 6-ethyl-3-[[3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]amino]-5-(oxan-4-ylamino)pyrazine-2-carboxamide | Human | 11802 | 0.40 | |
| TTK | TTK | Other | 3h9f | A | A | 9-cyclopentyl-2-(4-(4-hydroxypiperidin-1-yl)-2-methoxyphenylamino)-5-methyl-8,9-dihydro-5h-pyrimido[4,5-b][1,4]diazepin-6(7h)-one | Human | 4701 | 0.49 | |
| PLK1 | PLK | Other | 3fc2 | A | B | n-{trans-4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexyl}-4-{[(7r)-7-ethyl-5-methyl-8-(1-methylethyl)-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxybenzamide | Human | 4967 | 0.67 | |
| PLK1 | PLK | Other | 5ta8 | A | A | 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5h-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-3-methoxy-n-(1-methylpiperidin-4-yl)benzamide | Human | 7464 | 0.67 | |
| EGFR | EGFR | TK | 8h7x | A | | 5-chloro-n~4~-[2-(dimethylphosphoryl)phenyl]-n~2~-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}pyrimidine-2,4-diamine | Human | 14945 | 0.43 | |
| PLK2 | PLK | Other | 4i5m | A | | 4-{[(7r)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxy-n-(1-methylpiperidin-4-yl)benzamide | Human | 5557 | 1.00 | |
| EGFR | EGFR | TK | 7zym | A | | 5-chloro-n~4~-[2-(dimethylphosphoryl)phenyl]-n~2~-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}pyrimidine-2,4-diamine | Human | 14726 | 0.43 | |
| MERTK (MER) | Axl | TK | 7ab1 | A | | 6-ethyl-3-[[3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]amino]-5-(oxan-4-ylamino)pyrazine-2-carboxamide | Human | 12933 | 0.40 | |
| EGFR | EGFR | TK | 7aem | A | | 5-chloro-n~4~-[2-(dimethylphosphoryl)phenyl]-n~2~-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}pyrimidine-2,4-diamine | Human | 13482 | 0.43 | |
| PLK1 | PLK | Other | 2rku | A | B | 4-{[(7r)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxy-n-(1-methylpiperidin-4-yl)benzamide | Human | 4966 | 1.00 | |
| PLK1 | PLK | Other | 4j53 | A | A | 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5h-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-n-(1-methylpiperidin-4-yl)benzamide | Human | 4975 | 0.52 | |
| PLK1 | PLK | Other | 5ta6 | A | C | 4-{[(6r)-7-cyano-5-cyclopentyl-6-ethyl-5,6-dihydroimidazo[1,5-f]pteridin-3-yl]amino}-3-methoxy-n-(1-methylpiperidin-4-yl)benzamide | Human | 7463 | 0.73 | |
| PLK1 | PLK | Other | 4j53 | A | C | 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5h-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-n-(1-methylpiperidin-4-yl)benzamide | Human | 4963 | 0.52 | |
| PLK1 | PLK | Other | 4j52 | A | A | 4-{[(7r)-9-cyclopentyl-7-ethenyl-7-fluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5h-pyrimido[4,5-b][1,4]diazepin-2-yl]amino}-3-methoxy-n-(4-methylpiperazin-1-yl)benzamide | Human | 4955 | 0.53 | |
| PLK1 | PLK | Other | 5ta6 | A | A | 4-{[(6r)-7-cyano-5-cyclopentyl-6-ethyl-5,6-dihydroimidazo[1,5-f]pteridin-3-yl]amino}-3-methoxy-n-(1-methylpiperidin-4-yl)benzamide | Human | 7465 | 0.73 | |
| DYRK1A | DYRK | CMGC | 6eip | C | | 4-[[(3~{r},7~{s})-2-cyclopentyl-9-methyl-8-oxidanylidene-2,9,12,14-tetrazatricyclo[8.4.0.0^{3,7}]tetradeca-1(14),10,12-trien-13-yl]amino]benzamide | Human | 10533 | 0.48 | |
| TTK | TTK | Other | 5ap3 | A | | 9-cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8h-purin-8-one | Human | 6099 | 0.44 | |
| CAMKK2 (CaMKK2) | CAMKK | Other | 6bqq | A | | 4-{[(7r)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxy-n-(1-methylpiperidin-4-yl)benzamide | Human | 9063 | 1.00 | |
| CAMKK2 (CaMKK2) | CAMKK | Other | 6bql | A | | 2-({5-chloro-2-[(2-methoxy-4-morpholin-4-ylphenyl)amino]pyrimidin-4-yl}amino)-n-methylbenzamide | Human | 9061 | 0.40 | |
| DCLK1 | DCAMKL | CAMK | 7kxw | A | | 2-{[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino}-11-methyl-5-(2,2,2-trifluoroethyl)-5,11-dihydro-6h-pyrimido[4,5-b][1,4]benzodiazepin-6-one | Human | 13910 | 0.42 | |
| PTK2 (FAK) | FAK | TK | 6i8z | A | | 3-methoxy-~{n}-(1-methylpiperidin-1-ium-4-yl)-4-[[4-[(3-oxidanylidene-1,2-dihydroinden-4-yl)oxy]-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzamide | Human | 10904 | 0.44 | |
| PLK1 | PLK | Other | 3fc2 | A | A | n-{trans-4-[4-(cyclopropylmethyl)piperazin-1-yl]cyclohexyl}-4-{[(7r)-7-ethyl-5-methyl-8-(1-methylethyl)-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxybenzamide | Human | 4964 | 0.67 | |
| MAPK7 (Erk5) | MAPK | CMGC | 4b99 | A | | 11-cyclopentyl-2-[[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl-phenyl]amino]-5-methyl-pyrimido[4,5-b][1,4]benzodiazepin-6-one | Human | 388 | 0.55 | |
| TTK | TTK | Other | 5ap0 | A | | 9-cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8h-purin-8-one | Human | 6101 | 0.44 | |
| TTK | TTK | Other | 5ap7 | A | | n-(2,6-diethylphenyl)-1-methyl-8-({4-[(1-methylpiperidin-4-yl)carbamoyl]-2-(trifluoromethoxy)phenyl}amino)-4,5-dihydro-1h-pyrazolo[4,3-h]quinazoline-3-carboxamide | Human | 6100 | 0.46 | |
| Pik3cd (p110d) | PIK | Atypical | 6zaa | A | | 4-[6-methoxy-5-(methylsulfamoyl)pyridin-3-yl]-~{n}-(1-methylpiperidin-4-yl)-2,3-dihydro-1,4-benzoxazine-6-carboxamide | Mouse | 12635 | 0.40 | |
| MAPK7 (Erk5) | MAPK | CMGC | 5byy | A | B | 2-{[2-ethoxy-4-(4-hydroxypiperidin-1-yl)phenyl]amino}-5,11-dimethyl-5,11-dihydro-6h-pyrimido[4,5-b][1,4]benzodiazepin-6-one | Human | 6587 | 0.42 | |
| PLK1 | PLK | Other | 2rku | A | A | 4-{[(7r)-8-cyclopentyl-7-ethyl-5-methyl-6-oxo-5,6,7,8-tetrahydropteridin-2-yl]amino}-3-methoxy-n-(1-methylpiperidin-4-yl)benzamide | Human | 4969 | 1.00 | |
| PLK1 | PLK | Other | 4j53 | A | B | 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-6,7,8,9-tetrahydro-5h-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-n-(1-methylpiperidin-4-yl)benzamide | Human | 4972 | 0.52 | |
| PLK3 | PLK | Other | 4b6l | A | | 4-[[(4r)-5-cyclopentyl-4-ethyl-3a,4-dihydro-3h-[1,2,4]triazolo[4,3-f]pteridin-7-yl]amino]-n-cyclopropyl-3-methoxy-benzamide | Human | 3797 | 0.63 | |
| DYRK1A | DYRK | CMGC | 6eip | A | | 4-[[(3~{r},7~{s})-2-cyclopentyl-9-methyl-8-oxidanylidene-2,9,12,14-tetrazatricyclo[8.4.0.0^{3,7}]tetradeca-1(14),10,12-trien-13-yl]amino]benzamide | Human | 10555 | 0.48 | |
| DYRK1A | DYRK | CMGC | 6eip | D | | 4-[[(3~{r},7~{s})-2-cyclopentyl-9-methyl-8-oxidanylidene-2,9,12,14-tetrazatricyclo[8.4.0.0^{3,7}]tetradeca-1(14),10,12-trien-13-yl]amino]benzamide | Human | 10531 | 0.48 | |
| DYRK1A | DYRK | CMGC | 6eip | B | | 4-[[(3~{r},7~{s})-2-cyclopentyl-9-methyl-8-oxidanylidene-2,9,12,14-tetrazatricyclo[8.4.0.0^{3,7}]tetradeca-1(14),10,12-trien-13-yl]amino]benzamide | Human | 10517 | 0.48 | |
| CHEK1 (CHK1) | CAMKL | CAMK | 5oq5 | A | | 2-[(2-methoxy-4-{[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl}phenyl)amino]-5,11-dimethyl-5,11-dihydro-6h-pyrimido[4,5-b][1,4]benzodiazepin-6-one | Human | 8597 | 0.54 | |
| CHEK1 (CHK1) | CAMKL | CAMK | 5oot | A | | 2-[(2-methoxy-4-{[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl}phenyl)amino]-5,11-dimethyl-5,11-dihydro-6h-pyrimido[4,5-b][1,4]benzodiazepin-6-one | Human | 8599 | 0.54 | |
| MAP3K14 (NIK) | STE-Unique | STE | 6z1q | B | B | desf-3r/4076 | Human | 12449 | 0.45 | |
| MAP3K14 (NIK) | STE-Unique | STE | 6z1q | A | B | desf-3r/4076 | Human | 12454 | 0.45 | |
| MAP3K14 (NIK) | STE-Unique | STE | 6z1q | B | A | desf-3r/4076 | Human | 12455 | 0.45 | |
| PLK2 | PLK | Other | 4i6f | A | B | (7r)-8-cyclopentyl-7-ethyl-5-methyl-2-(2-phenyl-1h-imidazol-1-yl)-7,8-dihydropteridin-6(5h)-one | Human | 5563 | 0.45 | |
| ALK | ALK | TK | 6mx8 | A | B | 5-chloro-n~4~-[2-(dimethylphosphoryl)phenyl]-n~2~-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}pyrimidine-2,4-diamine | Human | 10799 | 0.43 | |
| ALK | ALK | TK | 6mx8 | A | A | 5-chloro-n~4~-[2-(dimethylphosphoryl)phenyl]-n~2~-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}pyrimidine-2,4-diamine | Human | 10798 | 0.43 | |
| TTK | TTK | Other | 5ntt | A | B | n-(2,6-diethylphenyl)-1-methyl-8-({4-[(1-methylpiperidin-4-yl)carbamoyl]-2-(trifluoromethoxy)phenyl}amino)-4,5-dihydro-1h-pyrazolo[4,3-h]quinazoline-3-carboxamide | Human | 8267 | 0.46 | |
| TTK | TTK | Other | 5mrb | A | | ~{n}-(2,6-diethylphenyl)-8-[[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamide | Human | 8270 | 0.41 | |
| TTK | TTK | Other | 2x9e | A | | n-(2,6-diethylphenyl)-1-methyl-8-({4-[(1-methylpiperidin-4-yl)carbamoyl]-2-(trifluoromethoxy)phenyl}amino)-4,5-dihydro-1h-pyrazolo[4,3-h]quinazoline-3-carboxamide | Human | 4729 | 0.46 | |
| TTK | TTK | Other | 7chm | A | | 4-(cyclohexylamino)-2-[(2-methoxy-4-morpholin-4-ylcarbonyl-phenyl)amino]-7h-pyrrolo[2,3-d]pyrimidine-5-carbonitrile | Human | 13550 | 0.44 | |
| TTK | TTK | Other | 5n87 | A | | ~{n}-(2,6-diethylphenyl)-2-[[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino]-5,6-dihydropyrimido[4,5-e]indolizine-7-carboxamide | Human | 7977 | 0.41 | |
| TTK | TTK | Other | 5ntt | A | A | n-(2,6-diethylphenyl)-1-methyl-8-({4-[(1-methylpiperidin-4-yl)carbamoyl]-2-(trifluoromethoxy)phenyl}amino)-4,5-dihydro-1h-pyrazolo[4,3-h]quinazoline-3-carboxamide | Human | 8268 | 0.46 | |
| TTK | TTK | Other | 5o91 | A | | ~{n}-(2,6-diethylphenyl)-8-[[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino]-1-methyl-4,5-dihydropyrazolo[4,3-h]quinazoline-3-carboxamide | Human | 8269 | 0.41 | |
| DCLK1 | DCAMKL | CAMK | 7kx6 | A | | 2-{[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino}-5,11-dimethyl-5,11-dihydro-6h-pyrimido[4,5-b][1,4]benzodiazepin-6-one | Human | 13907 | 0.45 | |
| DCLK1 | DCAMKL | CAMK | 7kxw | B | | 2-{[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino}-11-methyl-5-(2,2,2-trifluoroethyl)-5,11-dihydro-6h-pyrimido[4,5-b][1,4]benzodiazepin-6-one | Human | 13908 | 0.42 | |
| DCLK1 | DCAMKL | CAMK | 7kx8 | A | | 5-ethyl-2-{[2-methoxy-4-(4-methylpiperazin-1-yl)phenyl]amino}-11-methyl-5,11-dihydro-6h-pyrimido[4,5-b][1,4]benzodiazepin-6-one | Human | 13909 | 0.45 | |
| MAP3K14 (NIK) | STE-Unique | STE | 6z1q | A | A | desf-3r/4076 | Human | 12451 | 0.45 | |