Table 4.
CDK‐inhibitory activity of lead compound BAY‐958 and clinical candidate BAY 1143572 in the Merck Millipore KinaseProfilerTM panel.
| IC50 [nm] | BAY‐958 | BAY 1143572 |
|---|---|---|
| CDK9/CycT1(h) | 5 | 6 |
| CDK1/CycB(h) | 690 | 1100 |
| CDK2/CycE(h) | 470 | 1000 |
| CDK3/CycE(h) | 570 | 890 |
| CDK5/p35(h) | 800 | 1600 |
| CDK6/CycD3(h) | 4400 | >10 000 |
| CDK7/CycH/MAT1(h) | >10 000 | >10 000 |