Table 5.
Binding to human plasma and cell culture medium and calculated EC50s
| Compound | Mean % unbound in cell culture medium ± SDa | Calculated unbound EC50 (nM)b |
Mean % unbound in plasma ± SD | Calculated plasma-adjusted EC50 (nM)c |
||
|---|---|---|---|---|---|---|
| GT 1a | GT 1b | GT 1a | GT 1b | |||
| GS-9669 | 26.5 ± 0.7 | 2.9 | 0.7 | 1.50 ± 0.08 | 194 | 50 |
| Lomibuvir | 22.0 ± 7.6 | 2.9 | 1.3 | 0.64 ± 0.22 | 447 | 206 |
| Filibuvir | 30.3 ± 0.5 | 136 | 52 | 2.12 ± 0.59 | 6,395 | 2,432 |
a
By equilibrium dialysis versus phosphate buffer.
b
Unbound drug concentration at the observed EC50.
c
Total plasma concentration at the unbound EC50.