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2-Aminopyrimidines CDK9 inhibitors published by Aucentra Therapeutics.
|
||
|---|---|---|
| Compound | 33 | 34 |
| R | 3-Fluoroailin-1yl | Ph |
| R′ | F | Me |
| Ki (nM) | ||
| CDK9/T1 | 6 | 8 |
| CDK1/B | 70420 | 101530 |
| CDK2/A | 240 | 430 |
| CDK4/D1 | 691 | 2620 |
| CDK6/D3 | 1710 | 1540 |
| CDK7/H | 730 | 600 |
| GI50 (nM) | ||
| Cytotoxicity* | 0.24 | 0.61 |
CDK: cyclin-dependent kinase; GI50: half maximal inhibition of cell proliferation; Ki: inhibitory constant. *Average of 12 cell lines.
