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. Author manuscript; available in PMC: 2017 Sep 14.
Published in final edited form as: J Med Chem. 2016 Jan 22;59(11):5172–5208. doi: 10.1021/acs.jmedchem.5b01697

Table 2.

Resistance profile of inhibitor 14

Virusa EC50 values, nM (fold change)
14 DRV LPV
HIV-1r13205 26 22 28
HIV-1T20760 (14-selected) 65 (2.5) 39 (1.8) 112 (4.0)
HIV-1T21055 (14-selected) 308 (12) 122 (5.5) 426 (15)
HIV-1T21217 (14-selected) 312 (12) 84 (3.8) 198 (7.1)
HIV-1T13436 (DRV-selected) 5.1 (0.20) 49 (2.2) 263 (9.4)
HIV-1T13572 (DRV-selected) 1.5 (0.058) 234 (11) 511 (18)
HIV-1T13632 (DRV-selected) 42 (1.6) 624 (28) 1597 (57)
HIV-1T13717 (DRV-selected) 68 (2.6) 670 (30) 1900 (68)
a

Amino acid substitutions in the protease-encoding region compared to type r13205: L10F for T20760; L10F, I47V for T21055; L10F, I47V, L90M for T21217; V32I, L76V for T13436; V32I, L76V, V82I for T13572; V32I, I50V, L76V, V82I for T13632; V32I, I50V, G73S, L76V, V82I for T13727