Table 3.
Apparent IC50 values of substituted 2-(isoxazol-3-yl)-2-oxo-N′-phenyl-acetohydrazonoyl cyanide scaffolds for inhibiting EPAC2 GEF activity.
| Compound | Rap1b-bGDP EPAC2 IC50 (μM)a |
|---|---|
| 1 | 4.4 ± 0.5 |
| 10 | 2.2 ± 0.3 |
| 14 | 2.3 ± 0.5 |
| 15 | 3.3 ± 0.8 |
| 23 | 4.5 ± 1.0 |
| 24 | 7.0 ± 0.9 |
| 26 | 2.2 ± 0.3 |
| 27 | 2.3 ± 0.2 |
| 31 | 2.2 ± 0.2 |
| 32 | 2.2 ± 0.4 |
| 33 | 1.9 ± 0.3 |
The values are the mean ± SD of at least three independent experiments.