Table 1. Inhibitors of HCV NS3/4A.
| Compound | NCI identifier | NS3/4A docking site | NS3/4A NS2B-NS3 Furin | HCV replicon | ||||||
| WNV | DV2 | |||||||||
| IC50, µM | IC50, µM | IC90, µM | CC50, µM | CC90, µM | ||||||
| 1 | NSC704342 | 3 | 0.183 | 21.87 | 19.70 | >100 | >100 | >100 | >100 | >100 |
| 2 | NSC713288 | 2 | 0.3 | >100 | >100 | >100 | 10.02 | 25.19 | 9.99 | 22.06 |
| 3 | NSC724526 | 3 | 0.36 | 18.25 | 34.48 | >100 | >100 | >100 | >100 | >100 |
| 4 | NSC320254 | 3 | 0.36 | 3.7 | 14.33 | 12.76 | 27.99 | 99.4 | >100 | >100 |
| 5 | NSC724527 | 3 | 0.38 | 23.74 | 49.43 | >100 | >100 | >100 | >100 | >100 |
| 6 | NSC724525 | 3 | 0.95 | 12.74 | 20.59 | 66.79 | >100 | >100 | >100 | >100 |
| 7 | NSC716899 | 3 | 1.25 | 39.09 | >100 | >100 | 9.95 | 54.4 | 86.78 | 96.33 |
| 8 | NSC637712 | 3 | 1.92 | 21.77 | 38.80 | 26.97 | 13.6 | 19.2 | 14.23 | 26.61 |
NS3/4A activity was measured using Ac-DE-D(Edans)-EE-Abu-ψ-[COO]-AS-K(Dabsyl)-NH2 as a peptide substrate. The activity of furin and both WNV and DV2 NS2B-NS3 proteinases was measured using pyroglutamic acid-Arg-Thr-Lys-Arg-7-amino-4-methylcoumarin as a substrate. IC50 and IC90, compound concentrations, which reduced viral replication by 50% and 90%, respectively. CC50 and CC90, compound concentrations, which reduced cell viability by 50% and 90%, respectively. >100, determined values exceeded 100 µM. Refer to Table S1 for the compound structures.