TABLE 5.
EC90 multiple used for selectiona |
Inhibitor potency |
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---|---|---|---|---|---|---|---|---|---|
Elbasvir |
Grazoprevir |
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Grazoprevir | Elbasvir | EC50 |
EC90 |
EC50 |
EC90 |
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Value, nM | Fold shiftb | Value, nM | Fold shift | Value, nM | Fold shift | Value, nM | Fold shift | ||
0 | 0 | 0.002 | 1 | 0.003 | 1 | 1 | 1 | 2 | 1 |
0 | 1× | 0.3 | 150 | 2.4 | 800 | 1 | 1 | 2 | 1 |
0 | 10× | 0.5 | 250 | 2.3 | 767 | 1 | 1 | 1.2 | 0.6 |
0 | 100× | 5 | 2,500 | 22 | 7,333 | 1 | 1 | 2 | 1 |
0 | 1,000× | 36 | 18,000 | 63 | 21,000 | 1 | 1 | 2 | 1 |
1× | 0 | 0.003 | 1.5 | 0.004 | 1 | 2 | 2 | 10 | 5 |
10× | 0 | NTc | NT | NT | NT | 48 | 48 | 92 | 46 |
1× | 1× | 0.04 | 20 | 1 | 333 | 4 | 4 | 7 | 3.5 |
1× | 10× | 1.3 | 650 | 4.6 | 1,533 | 2 | 2 | 3 | 1.5 |
EC90 multiples used for GT1a(H77) selection: grazoprevir EC90, 1.5 nM; elbasvir EC90, 6 pM.
Change in potency relative to the DMSO (0×/0×) control.
NT, not tested.