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. Author manuscript; available in PMC: 2018 Jul 7.
Published in final edited form as: Eur J Med Chem. 2017 Apr 4;134:62–71. doi: 10.1016/j.ejmech.2017.04.001

Table 2.

Apparent IC50 values of substituted 2-(isoxazol-3-yl)-2-oxo-N′-phenyl-acetohydrazonoyl cyanide scaffolds for inhibiting EPAC1 GEF activity.

graphic file with name nihms867091u3.jpg
Compound R2 Rap1b-bGDP EPAC1 IC50 (μM)a
30 3-Cl 13.2 ± 3.6
31 3-Cl, 5-CF3 4.6 ± 0.8
32 3-Cl, 4-CF3 3.0 ± 0.3
33 3-CF3, 4-Cl 2.7 ±0.3
34 3-Cl, 5-F 18.9 ± 4.9
35 3-Cl, 4-F 8.5 ± 3.5
36 3,5-di-CF3 6.7 ± 0.7
37 3,4,5-tri-F 13.1 ± 2.5
a

The values are the mean ± SD of at least three independent experiments.