FIG 1.
Structure of GSK’254 and MI EC90 against a minilibrary of clinically relevant HIV-1 polymorphisms in a multiple-cycle assay. (A) Structure of GSK’254. The C-20/C-30 double bond that was reduced to make radiolabeled surrogate maturation inhibitors is shown. (B) PBA EC90 of GSK’254 and GSK’795 against a minilibrary of HIV-1 polymorphisms. The estimated Cmin for GSK’254 was 150 nM, as represented by the red dashed line. Mean values and standard errors of the means are graphed for each MI. The mean value for GSK’795 was calculated using 3 fewer samples, as 3 viruses did not have a measurable EC90 (V362I/V370A- and A326T/V362I/V370A-containing viruses and a virus containing the 93BR024 gag/pro gene). Cmin, steady-state serum concentration; EC90, 90% effective concentration; GSK’254, GSK3640254; GSK’795, GSK3532795; MI, maturation inhibitor; PBA, protein-binding adjusted.