Table 1 Kinase profiling using selected TNKS inhibitors at 10 μM. Dose response was measured for selected kinase-inhibitor pairs and inhibition-% or an IC50 is shown.
From: 2-Phenylquinazolinones as dual-activity tankyrase-kinase inhibitors
Compound | CDK9 | Akt | p42 | p38 | GSK3β | CK2 | TNKS2 |
|---|---|---|---|---|---|---|---|
| 34% | 1% | 14% | 3% | 57% | 12% | 400 nM |
| 31% | 2% | 3% | 3% | 11% | 1% | 15 nM |
| 16% | 48% | 18% | 20% | 4% | 2% | 10 nM |
| 6.2 µM | 14.7 µM | — | — | — | — | 660 nM |
| 16.1 µM* | 13.3 µM | — | — | — | — | 16 nM |
| 3.4 µM | 1.6 µM | 51% | 45% | 41% | 2% | 1,050 nM |
| 28.3 µM* | 13.8 µM | — | — | — | — | 145 nM |
| 12% | 7% | 2% | 3% | 7% | 1% | 5 nM |
| 9% | 1% | 3% | 3% | 3% | 1% | 25 nM |
