Table 1. IC50 values for compounds in the CDK enzyme assaysa,b.
IC50 (μM) |
||||||
---|---|---|---|---|---|---|
X1 | X2 | CDK4/Cyclin D1 | CDK6/Cyclin D3 | CDK1/Cyclin B | CDK2/Cyclin A | |
2 | N | CH | 0.006 ± 0.001 | 0.049 ± 0.006 | 1.2 ± 0.2 | 0.27 ± 0.06 |
3 | N | N | 0.012 ± 0.002 | 0.3 ± 0.1 | >15 | 6.2 ± 0.4 |
4 | CCN | N | 0.003 ± 0.000 | 0.026 ± 0.003 | 5.6 ± 0.4 | 2.4 ± 0.2 |
5 | N | CH | 0.25 ± 0.03 | NT | >15 | >15 |
6 | CCN | N | 0.015 ± 0.001 | 0.12 | >15 | >15 |
Results are expressed as the mean ± standard deviation of 1–2 IC50 determinations. For each determination, concentration–inhibition curves were obtained in duplicate and then averaged to afford a single IC50 curve with a ≥95% confidence interval.
70% homology shared between CDK4 and -6 contributes to comparable SAR profiles of two enzymes.