Primary screening (% of residual activity at 10 mM and 1 mM) | |||||||||
Compound | Conc. (mM) | CDK5/ p25 | CDK9/ cyclin T | CK1e | GSK3b | Haspin | PIM1 | CLK1 | DYRK1A |
5a | 10 | ≥100 | 96 | 60 | 79 | 55 | 96 | 80 | 71 |
1 | 98 | 76 | 65 | 82 | 91 | 84 | 88 | 99 | |
5b | 10 | 98 | 84 | 78 | 85 | 68 | 97 | 78 | ≥100 |
1 | 95 | 61 | 52 | 90 | ≥100 | 99 | 87 | 85 | |
5c | 10 | 98 | 72 | 63 | 78 | 60 | 72 | 90 | 90 |
1 | 94 | 57 | 44 | 72 | 45 | 81 | 80 | 58 | |
5d | 10 | 91 | 51 | 38 | 65 | 34 | 79 | 81 | 82 |
1 | 94 | 54 | 57 | 82 | 51 | 78 | 75 | 57 | |
6a | 10 | 86 | 62 | 58 | 66 | 46 | 52 | 51 | 34 |
1 | ≥100 | 60 | 63 | 74 | 67 | 84 | 83 | 71 | |
6b | 10 | 76 | 57 | 47 | 71 | 53 | 68 | 74 | 65 |
1 | 86 | 50 | 42 | 65 | 90 | 92 | 75 | 67 | |
6c | 10 | 80 | 43 | 46 | 55 | 38 | 72 | 81 | 74 |
1 | 89 | 54 | 59 | 64 | 71 | 80 | 71 | 78 | |
6d | 10 | 87 | 38 | 39 | 31 | 31 | 76 | 61 | ≥ 100 |
1 | 89 | 63 | 67 | 78 | 66 | 77 | 71 | 88 |