Figure 1: Kinetic measurement of clinical inhibitors.

Kinetic inhibition dose-response curves of 8 clinical protease inhibitors for PRS5B proteolytic activity of FRET-based substrate. Reaction carried out in 50 mM MES pH 5.6, 200 mM sodium chloride, 0.5 mM EDTA, and 2.5% glycerol at 37°. Coefficient of determination for the regression (R²) and replicate K_i value are shown. K_i was calculated as K_i = (IC50 − [E]/2)/(1 + [S]/K_m). Final K_i values are mean ± SD (n=3–5).