Table 1.

Mutations and antiviral phenotype of replicons obtained following culturing in the presence of BILN 2061^a using various selection protocols

Antiviral pressure (fold EC50)	Fold increaseb compared to WT	EC50 ± SDb (μM)	NS3 mutation(s) (aa 22-336)c	Critical phased
1	2	0.033 ± 0.008	S174S/C	N
2	16	0.24 ± 0.08	D168D/E/V, S174S/C	N
5	13	0.19 ± 0.09	D168D/E/V, S174S/C	N
25	67	1 ± 0.4	D168V, E176E/G	Y
125	200	3 ± 0.5	D168V, S174S/C, E176E/G	Y
2-5	17	0.26 ± 0.007	D168D/E/V, S174S/C	N
2-25	61	0.92 ± 0.3	D168V, S174S/C, E176E/G	N
2-125	133	2 ± 0.2	D168V, S174S/C, E176E/G	N
5-25	56	0.84 ± 0.005	D168D/V, S174S/C, E176E/G	N
5-125	133	2 ± 0.6	D168V, S174S/C, E176E/G	N
25-125	133	2 ± 0.3	D168V	N
2-5-25	133	2 ± 0.6	D168V, S174S/C	N
2-5-125	133	2 ± 0.6	D168V, S174S/C	N
2-25-125	133	2 ± 0.5	D168V, S174S/C, S280S/A	N
5-25-125	200	3 ± 0.04	D168V, S174S/C, E176E/G, S280S/A	N
2-5-25-125	267	4 ± 0.7	D168V, S174S/C	N

^aEC₅₀, 0.015 ± 0.01 μM; CC₅₀, 22.6 ± 0.1 μM.

^bData are mean values for 2 independent determinations of the antiviral phenotype.

^cMajor resistance mutations are indicated in boldface. aa, amino acids.

^dY, yes; N, no.