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. Author manuscript; available in PMC: 2009 Jul 6.
Published in final edited form as: J Med Chem. 2008 May 29;51(12):3378–3387. doi: 10.1021/jm7015478

Figure 5.

Figure 5

Screening of compounds for the inhibition of ECE-2 activity. (A) The rate of McaBk2 fluorescent substrate hydrolysis by recombinant ECE-2 was measured in the absence and presence of 10μM of each of forty top scoring compounds by initial screening. Data are represented as % activity of ECE-2 without inhibitor. Two most potent compounds, 1 and 2 inhibited ECE-2 activity by more than 70%. (B) Concentration-dependent inhibition curves for selected inhibitor compounds, 1 and 2, were generated by measuring substrate hydrolysis in the presence of inhibitors at concentrations 1nM-1mM. (C) IC50 values for each selected inhibitor compound were determined for ECE-2 and NEP by establishing concentration-dependent inhibition curves for a final McaBk2 concentration of 10μM. Data represent the mean±SEM (n=5).