Skip to main content
. Author manuscript; available in PMC: 2018 Dec 1.
Published in final edited form as: Bioorg Med Chem Lett. 2017 Oct 25;27(23):5163–5166. doi: 10.1016/j.bmcl.2017.10.056

Table 2.

IC50 values of substituted 2-phenyl-N-(3,5-dichlorophenyl)-2-oxoacetohydrazonoyl cyanides for inhibiting EPAC1/2 GEF activity.

graphic file with name nihms917591u3.jpg
Entry R or X Rap1b-bGDP EPAC1 IC50 (μM)a Rap1b-bGDP EPAC2 IC50 (μM)
10 4-tert butyl 5.4 ± 0.7 2.5 ± 0.6
22 4-Cl >300 NDb
23 3-Cl >300 ND
24 4-OCF3 40.9 ± 6.8 ND
25 4-CO2Me 29.3 ± 6.2 ND
26 4-Ph >300 ND
27 3,4-di OMe >300 ND
28 4-Piperidin-1-ylmethyl 39.4 ± 4.7 ND
29 4-Morpholinomethyl 14.6 ± 5.7 ND
30 4-Cyclohexane 32.4 ± 9.5 ND
31 graphic file with name nihms917591t1.jpg 3.6 ± 0.3 1.2 ± 0.1
32 graphic file with name nihms917591t2.jpg 11.3 ± 1.4 2.5 ± 0.5
33 graphic file with name nihms917591t3.jpg 19.6 ± 6.7 ND
a

The values are the mean ± SE.

b

ND: not determined.