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Integrase Inhibitory Potencies In Vitro Using Wild-Type (WT) and Mutant Enzymes.a
| No. | ST IC50 (μM, WT) | Mutantsb |
||
|---|---|---|---|---|
| G140S/Q148H | Y143R | N155 H | ||
| 1 | 0.067 | 105 x | 26 x | 7 x |
| 4b-1 | 9.1 ± 1.1 | 6 x | 2 x | 3 x |
Data was obtained from in vitro IN assays using Mg2+ cofactor as described in the Supporting Information.
Fold-loss of potency relative to WT enzyme for ST.
