Table 1.
Kinase panel profiling of indolyl pyrimidinamine library.
 | ||||||||
|---|---|---|---|---|---|---|---|---|
| Compound | Scaffold | n | R | TTBK1 PoC/enzymatic IC50 (nM) | TTBK2 PoC/enzymatic IC50 (nM) | # kinases < 10 PoC in enzyme panel | S10(1 μM)[a] | # scanMAX kinases with PoC < 10[b] |
| 1 | A | 1 |  |
78/3140 | 43/1210 | 2 | 0.05 | 20 |
| AMG28 | A | 2 |  |
50/805 | 20/988 | 7 | 0.052 | 21 |
| 2 | A | 3 |  |
92/NT[c] | 69/NT | 1 | NT | NT |
| 3 | B | N/A[d] |  |
43/816 | 24/384 | 3 | 0.084 | 34 |
| 4 | A | 2 |  |
78/NT | 64/NT | 1 | NT | NT |
| 5 | A | 2 |  |
68/NT | 72/NT | 6 | NT | NT |
| 6 | A | 2 |  |
91/NT | 76/NT | 3 | NT | NT |
| 7 | A | 2 |  |
86/NT | 104/NT | 1 | NT | NT |
| 8 | A | 2 |  |
85/NT | 103/NT | 1 | NT | NT |
| 9 | A | 2 |  |
41/384 | 17/175 | 2 | 0.017 | 7 |
| 10 | A | 2 |  |
37/579 | 18/258 | 3 | 0.055 | 22 |
| 11 | A | 2 |  |
117/NT | 110/NT | 1 | NT | NT |
aS10(1 μM): percentage of screened kinases with percent of control (PoC) values < 10 at 1 μM. bNumber of kinases with PoC values < 10 at 1 μM. cNT: not tested. dN/A: not applicable.