TABLE 8.

K_i values of potent HIV-1 PR inhibitors against the F12s and F21s mutants^a

Proteaseb	Ki (nM)
	Saquinavir	Ritonavir	Nelfinavir	JE-2147
FIV
Wild type	>45,000	>45,000	>30,000	>45,000
F12s	37	15	29	NAc
F21s	25	44	16	18
HIV-1	3	2	3	3

^aData were obtained at pH 5.6 in 0.1 M NaH₂PO₄-0.1 M sodium citrate-1.5 M NaCl-0.1 mM dithiothreitol-5% glycerol. The K_i values were derived from IC₅₀ values with the equation K_i = IC₅₀/(1 + [S]/K_m).

^bF12s, 37³²/55⁴⁶/56⁴⁷/57⁴⁸/59⁵⁰/62⁵³/63⁵⁴/97⁸⁰/98⁸¹/99⁸²/100⁸³/101⁸⁴; F21s, F12s plus 35³⁰/54⁴⁵/64⁵⁵/65⁵⁶/66⁵⁷/67⁵⁸/88⁷⁴/90⁷⁶/105⁸⁸.

^cNA, not assayed.