Table 2.
Inhibitory activities of compounds 4a-t against CDK9 and CDK12
| Compound | IC50 (μM) | |
|---|---|---|
| CDK9 | CDK12 | |
| 4a | 0.396 ± 0.017 | 0.295 ± 0.011 |
| 4b | 1.15 ± 0.05 | 0.566 ± 0.022 |
| 4c | 0.041 ± 0.002 | 0.14 ± 0.005 |
| 4 d | 0.782 ± 0.034 | 1.329 ± 0.052 |
| 4e | 0.409 ± 0.018 | 0.425 ± 0.017 |
| 4f | 0.762 ± 0.033 | 1.143 ± 0.044 |
| 4 g | 0.114 ± 0.005 | 0.071 ± 0.003 |
| 4 h | 0.05 ± 0.002 | 0.153 ± 0.006 |
| 4i | 1.088 ± 0.047 | 0.365 ± 0.014 |
| 4j | 0.055 ± 0.002 | 0.104 ± 0.004 |
| 4k | 5.468 ± 0.236 | 1.211 ± 0.047 |
| 4 l | 1.673 ± 0.072 | 0.899 ± 0.035 |
| 4 m | 0.04 ± 0.002 | 0.06 ± 0.002 |
| 4n | 0.392 ± 0.017 | 0.179 ± 0.007 |
| 4o | 1.045 ± 0.045 | 1.876 ± 0.073 |
| 4p | 0.153 ± 0.007 | 0.664 ± 0.026 |
| 4q | 0.057 ± 0.002 | 0.074 ± 0.003 |
| 4r | 0.242 ± 0.01 | 0.104 ± 0.001 |
| 4 s | 0.408 ± 0.018 | 0.189 ± 0.007 |
| 4 t | 0.121 ± 0.005 | 0.533 ± 0.021 |
| Dinaciclib | 0.032 ± 0.001 | % 1.% 2 ± 0.002 |