Effects of resistance mutations on the inhibitory activity of compounds 1–8.

The IC50 values of the compounds were determined in the cleavage assays in vitro using the recombinant wild-type (WT) and mutant (V36M, R155K, A156T, D168A and V170A) NS3/4A constructs and Ac-DE-D(Edans)-EE-Abu-ψ-[COO]AS-K(Dabcyl)-NH2 as a substrate.¥The IC50 was directly measured in vitro using the purified recombinant WT and mutant NS3/4A constructs [75].*The IC50 was measured using the mutant HCV replicon with luciferase readout [9], [14], [15]. FC, the fold change in the IC50 for the mutant compared to that the WT proteinase. ND, not determined, n/a, not applicable.