Figure 4. Selected compounds efficiently inhibit the catalytic activity of NS3/4A: representative dose-response curves.

Before the addition of the Ac-DE-D(Edans)-EE-Abu-ψ-[COO]-AS-K(Dabsyl)-NH₂ substrate (10 µM), NS3/4A (10 nM) was co-incubated for 30 min at ambient temperature with increasing concentrations of compounds 1, 4 and 7. The residual activity was then monitored continuously at λ_ex = 355 nm and λ_em = 500 nm to determine the initial velocity of the reactions. The initial velocity was calculated as a percentage of residual activity versus the untreated proteinase (control). Refer to Table S1 for the compound structures.