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2-Aminopyrimidines CDK9 inhibitors published by Changzhou Le Sun Pharmaceuticals.
|
|||
|---|---|---|---|
| Compound | 11 (CDKI-73) | 12 | 13 |
| R | Me | H | Me |
| X | F | F | Cl |
| Ki (nM) | |||
| CDK9/T1 | 4 | 3 | 10.5 |
| CDK1/B | 4 | 7 | 19 |
| CDK2/A | 3 | 3 | 10 |
| CDK5/p35 | 0.5 | 1.5 | 1.5 |
| CDK6/D3 | 167 | 116 | 87.5 |
| CDK7/H | 91 | 87 | 695 |
| GI50 (nM) | |||
| Cytotoxicity* | 30 | 225 | 75 |
CDK: cyclin-dependent kinase; GI50: half maximal inhibition of cell proliferation; Ki: inhibitory constant. *Average of two cell lines.
