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Pyridines CDK9 inhibitors published by AstraZeneca.
| Compounds* | CDK9 (IC50, nM) ATP conc. At Km | CDK9 (IC50, nM) high ATP conc. | Phospho-RNAPolyII Ser2 (IC50, nM) | Caspase activity MV4-11 (IC50, nM) |
|---|---|---|---|---|
| 42 | <3 | <3 | <7 | 13 |
| 43 | <3 | <4 | 11 | 15 |
| 44 | <3 | <3 | 10 | 15 |
| 45 | <3 | <3 | 7 | 10 |
| 46 | <3 | 9 | 38 | 36 |
CDK: cyclin-dependent kinase; IC50: half maximal inhibitory concentration; Phospho-RNAPolyII: phosphorylated RNA polymerase II. *From the corresponding structures in Figure 6.
