Table 2.
Selectivity of 4a and 16aa
| Kinase | 4a | 16a | Kinase | 4a | 16a |
|---|---|---|---|---|---|
| ABL | −4 | 6 | IRAK4 | 16 | 5 |
| AKT1 | −9 | 6 | JAK2 | 15 | 18 |
| AKT2 | 3 | −1 | JNK2 | 4 | 14 |
| AKT3 | 7 | 3 | KDR | 14 | −4 |
| AMPK | 2 | 7 | LCK | 2 | 3 |
| AurA | 6 | 4 | LYN | 3 | 8 |
| BMX | 8 | 10 | MAPKAPK2 | 0 | 5 |
| BTK | 10 | 7 | MARK1 | 5 | −6 |
| CAMK2 | −6 | −1 | MET | 3 | −6 |
| CAMK4 | 10 | −8 | MSK1 | −3 | −1 |
| CDK2 | 0 | −2 | MST2 | 2 | 1 |
| CHK1 | −10 | −20 | p38α | −2 | 0 |
| CHK2 | 1 | 4 | p70S6K | 10 | 8 |
| CK1δ | 3 | 7 | PAK2 | 3 | −1 |
| c-Raf | 9 | −1 | PDGFRα | 7 | 6 |
| c-TAK1 | 5 | 0 | PDK1 | 17 | 1 |
| DYRK1α | 20 | 68 | PIM1 | 73 | 36 |
| EGFR | −1 | −3 | PIM2 | 68 | 62 |
| Erk1 | 2 | 1 | PKA | 2 | 3 |
| Erk2 | 4 | −1 | PKCβ2 | −2 | −1 |
| FGFR1 | 3 | 1 | PKCζ | −2 | 3 |
| FLT1 | 18 | NT | PKD2 | −6 | −3 |
| FLT3 | −2 | 1 | PKGα | 1 | 0 |
| FLT3(D835Y) | 12 | 9 | PLK1 | 3 | 9 |
| FYN | 3 | 0 | PRAK | −3 | 4 |
| GSK3β | −1 | 3 | ROCK2 | 5 | 5 |
| HGK | −14 | 9 | RSK1 | 3 | 5 |
| IGF1R | 1 | −1 | SGK1 | 0 | 5 |
| Ikkβ | 12 | 10 | SRC | 4 | 4 |
| INSR | 5 | 4 | SYK | 5 | −3 |
a
The effects of 4a or 16a on the indicated protein kinases were determined through the Rapid Kinase Advisor profiling service from Caliper Life Sciences. Values represent the percent inhibition of each kinase at 5 µM of the test compound