Table 3. Apparent IC50 Values of Substituted 2-(Isoxazol-3-yl)-2-oxo-N′-phenyl-acetohydrazonoyl Cyanide Scaffolds with Modifications on the Linker for Competing with 8-NBD-cAMP in Binding to EPAC2.
| |||
---|---|---|---|
Compd | Linker | R3 | IC50 (μM)a |
1 | t-Bu | 8.9 | |
51 | Me | NEb | |
52 | t-Bu | NE | |
53 | t-Bu | NE | |
54 | t-Bu | NE | |
55 | t-Bu | NE | |
56 | t-Bu | NE | |
57 | t-Bu | NE |
The values are the mean ± SE of at least three independent experiments.
NE: no effect, indicating that a specific IC50 cannot be calculated from the data points collected.