Compoundsj EC50 (nM) Fold-Change in EC50 Relative to HIV-1 IIIb
HIV-1 IIIb T66Ia L74Mb E92Qc E92Vd E138Ke Q148Kf V151Ag N155Hh N155Si L74M/ E92V E92V/ V151A E138K/Q148K E92V/G140S/V151A
RAL 4.3 1.9 1.7 6 7 1 136 4 24 43 15 31 747 166
GS-9160 1.7 1.9 1 26 17 1 28 10 61 36 56 126 676 689
GS-9224 5.6 1 1 21 7 1 42 5 110 65 25 73 419 438
a Selected by L-708,906 (30, 32), S-1360 (31, 33) and EVG (37).
b Selected by GS-9224 (this report), L-708,906 (32), S-1360 (33), L-870,810 (42) and GS-9160 (19).
c Selected by EVG (31) and L-870,810 (42).
d Selected by GS-9160 (19).
e Selected by S-1360 (33).
f Selected by GS-9224 (this report), S-1360 (31) and RAL (14, 39).
g Selected by GS-278012, an analog of GS-9160 (19).
h Developed in SHIV (89.6P) infected Rhesus macaques treated with L-870,812 (34).
i Selected by S-1360 (31).
j The EC50 and fold-change represent the mean of a least two independent experiments performed in triplicate.
Table 4: Resistance Profile of Mutant Viruses Conferring Resistance to INSTIs.
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