Table 2. NanoBRET Profiling of Entire Aminopyrimidine Library.
| IC50 values (nM) |
||||
|---|---|---|---|---|
| compound | DRAK1b | MARK3c | MARK4c | TBK1b |
| 3 | >10000 | >10000 | >10000 | >10000 |
| 4 | 874 ± 103 | >10000 | >10000 | 2680 ± 230 |
| 5 | >10000 | >10000 | >10000 | 7456 |
| 6 | >10000 | >10000 | >10000 | >10000 |
| 7 | 126 ± 27.6 | >10000 | 3537 | 321 ± 2.49 |
| 8 | >10000 | >10000 | >10000 | >10000 |
| 9 | 638 ± 91.1 | 872 | 214 | >10000 |
| 10 | >10000 | >10000 | 8445 | >10000 |
| 11 | >10000 | >10000 | >10000 | 2050 ± 196 |
| 12 | >10000 | >10000 | >10000 | >10000 |
| 13 | >10000 | >10000 | >10000 | 6170 ± 2190 |
| 14 | 3622 | 4015 | 808 | >10000 |
| 15 | >10000 | >10000 | >10000 | >10000 |
| 16 | >10000 | >10000 | >10000 | >10000 |
| 17 | 2311 | >10000 | >10000 | >10000 |
| 18 | 4.47 ± 0.406 | 137 | 72 | 338 ± 22.5 |
| 19 | >10000 | >10000 | >10000 | >10000 |
| 20 | >10000 | >10000 | >10000 | >10000 |
| 21 | >10000 | >10000 | >10000 | >10000 |
| 22 | 58.2 ± 3.21 | 2001 | 509 | 2580 ± 215 |
| MRT67307 | 43.2 ± 2.69 | 328 ± 38.5 | 319 | N.T.a |
| MRT68921 | N.T.a | 95 | N.T.a | N.T.a |
| BX-795 | N.T.a | 515 | N.T.a | N.T.a |
| BX-912 | N.T.a | 3333 | 338 ± 4.5 | 2327 |
| GSK8612 | >10000 | >10000 | >10000 | 339 ± 39.5 |
a
N.T.: not tested.
b
Compounds tested in singlicate (n = 1) in dose–response where error not shown, and compounds with SEM tested in triplicate (n = 3) in dose–response.
c
Compounds tested in singlicate (n = 1) in dose–response where error not shown, and compounds with SEM tested in duplicate (n = 2) in dose–response.