Table 8.
Kinase selectivity of chemical probe (11s)
| KINOMEscan a | Enzyme b | NanoBRET c | ||
|---|---|---|---|---|
| Kinase | % I | KD | IC50 (nM) | IC50 (nM) |
| MET | 100 | >10,000 | >10,000 | — |
| NEK6 | 100 | >10,000 | >10,000 | — |
| PIM2 | 100 | 1500 | >10,000 | — |
| WEE1 | 100 | >10,000 | >10,000 | — |
| STK17B | 99 | 5.6 | 34 | 190 |
| CAMKK2 | 92 | 21 | >10,000 | 2,400 |
| AURKB | 86 | 110 | 8900 | >10,000 |
| CAMKK1 | 86 | 49 | 5200 | — |
| STK38L | 71 | >10,000 | >10,000 | >10,000 |
| STK17A | 27 | 440 | 4700 | >10,000 |
a
DiscoverX KINOMEscan. % I, scanMAX % inhibition of control at 1 μM, n = 1. KD, determined by dose response, n = 2.
b
IC50 for enzyme inhibition at Km ATP determined at Eurofins, n = 2.
c
Target engagement IC50 determined by NanoBRET assay in HEK293 cells. — not determined.