Table 4.
In-vitro CDK5/p25 and CDK2/E assay
| Compound # | CDK5/p25 % inhibitiona @ 50 μM | CDK2/E % inhibitiona @ 50 μM | CDK5/p25 IC50 (μM)b | CDK2/E IC50 (μM)b |
|---|---|---|---|---|
| 5 | 20.0 | 24.2 | ||
| 6 | 43.1 | 32.3 | ||
| 7 | 23.6 | 29.9 | ||
| 8 | 12.7 | 14.8 | ||
| 9 | 25.2 | 38.7 | ||
| 10 | 88.2 | 77.0 | 7.02 | 25.8 |
| 11 | 17.2 | 8.0 | ||
| 12 | 48.3 | 58.2 | 107 | 81.7 |
| 13 | 14.7 | 5.3 | ||
| 14 | 64.8 | 23.5 | 52.1 | 14.5% inhc |
| 1 | 0.188 | 0.028 | ||
| 4 | 0.655 | 0.417 |
a
At least two independent experiments were performed to generate the average numbers @ 10 μM ATP and 50 μM compound concentrations
b
Assays were performed @ ATP (Km) concentrations of 30 μM for CDK5/p25 and 65 μM for CDK2/E and at least two independent experiments were performed to generate the average values
c
% inhibitions were generated @ 50 μM compound and ATP Km concentrations