Table 9. Selectivity Profiles of Lead Compoundsa.
| compound | DYRK1A | DYRK1B | DYRK2 | CLK1 | CLK2 | CLK3 | CDK2 | GSK3β | S score (35) |
|---|---|---|---|---|---|---|---|---|---|
| 11 | 0.4 | 2.7 | 19 | 7.1 | 9.4 | 54 | 100 | 94 | 0.027 |
| 12 | 34 | 43 | 100 | 79 | 95 | 96 | 100 | 91 | 0.013 |
| 22 | 0.7 | 8.3 | 11 | 33 | 13 | 54 | 100 | 75 | 0.042 |
| 24 | 33 | 81 | 66 | 71 | 61 | 100 | 100 | 92 | 0.004 |
| 28 | 2.4 | 7.2 | 15 | 17 | 16 | 88 | 100 | 77 | 0.050 |
| 29 | 1.5 | 9.1 | 25 | 16 | 15 | 73 | 95 | 100 | 0.035 |
| 31 | 20 | 34 | 39 | 48 | 62 | 96 | 95 | 98 | 0.011 |
| 33 | 1.7 | 18 | 29 | 36 | 72 | 95 | 100 | 100 | 0.027 |
| 34 | 1.3 | 10 | 28 | 47 | 51 | 89 | 86 | 100 | 0.032 |
| 63 | 1.1 | 1.6 | 25 | 15 | 13 | 76 | 89 | 100 | 0.027 |
| 66 | 0.2 | 0.7 | 24 | 7.8 | 12 | 83 | 100 | 100 | 0.022 |
| 70 | 0.7 | 6.2 | 35 | 20 | 31 | 56 | 86 | 77 | 0.022 |
| 95 | 18 | 71 | 55 | 53 | 54 | 84 | 100 | 93 | 0.002 |
% Remaining activity as determined by DiscoverX KINOMEscan experiment. Inhibitor concentration = 1 μM.