Figure 1: Characterization of the compounds.
From: Inhibition of delta-secretase improves cognitive functions in mouse models of Alzheimer’s disease
(a) Chemical structure of the top 8 candidates. (b) IC50 values of the compounds towards δ-secretase, cathepsin-S, cathepsin-L, caspase-3 and caspase-8 (mean±s.d.). (c) IC50 values of the compounds towards δ-secretase in Pala cells (mean±s.d.). (d) Steady-state kinetic parameters were determined by varying substrate, Z-AAN-AMC, at fixed concentrations of compound 11. KI value was determined by global fits to the competitive inhibition equation. (e) Time course inactivation assays were used to generate progress curves, depicting product formation as a function of time. Pseudo first-order rate constants were obtained at each concentration of compound 11. (f) Re-plot of the pseudo first-order rate constants, kobs, versus the concentration of compound 11.
