Table 2.
Kinase profiling of compound 1zb (1 µM) against a 30-kinase panel. The results are expressed as mean %inhibition ± SEM
| Kinase | % inhibition |
|---|---|
| ABL | 7.57% ± 2.5% |
| ALK | 41.16% ± 1.5% |
| A-RAF | 9.14% ± 1.0% |
| Aurora-A | 49.77% ± 5.5% |
| B-RAFwt | 23.37% ± 0.9% |
| BTK | 16.96% ± 0.8% |
| DMPK | 0.84% ± 0.1% |
| EGFR | 19.93% ± 2.0% |
| ErbB2 | 2.17% ± 0.9% |
| ErbB4 | 13.67% ± 2.8% |
| FLT3 | 73.14% ± 2.0% |
| FMS | 12.19% ± 0% |
| JAK1 | −0.26% ± 0% |
| JAK2 | 3.76% ± 0.5% |
| JNK1(α1) | 0.76% ± 0.1% |
| KDR | 18.76% ± 1.0% |
| cKIT | 9.63% ± 0% |
| LCK | 12.45% ± 2.5% |
| MEK1 | 1.50% ± 0.2% |
| MEK2 | 26.60% ± 2.5% |
| mTOR | 7.83% ± 0.3% |
| PDGFRβ | 12.54% ± 1.5% |
| PI3Kα | 5.85% ± 0% |
| PI3K-C2α | 49.99% ± 2.3% |
| ROS | 2.02% ± 0.3% |
| Src(T341M) | 1.57% ± 0.3% |
| STK33 | 15.65% ± 0.5% |
| TRKA | 46.72% ± 1.5% |
| VRK1 | 3.93% ± 0.5% |
| V600E-B-RAF | 99.48% ± 0.09%a |
aData taken from Table 1.