TABLE 2.

Effects of AD101 and SCH-C on HIV-1 entry mediated by CCR5 TM mutants^a

TM	Mutant	Relative % entry in presence ofb:
		AD101	SCH-C
TM1	L33	34.2 ± 2.2	19.9 ± 2.7
	Y37	71.5 ± 2.2	32.1 ± 5.5
	F41	2.6 ± 1.9	4.3 ± 0.8
	N48	0.0 ± 0.0	0.0 ± 0.0
	L55	1.8 ± 2.7	0.0 ± 0.0
	I56	0.7 ± 3.0	0.0 ± 0.0
TM2	Y68	NA	NA
	L69	0.0 ± 0.0	0.0 ± 0.0
	N71	0.0 ± 0.0	0.0 ± 0.0
	D76	44.7 ± 5.1	20.6 ± 3.3
	F79	30.1 ± 6.2	0.0 ± 0.0
	T82	0.8 ± 2.0	0.0 ± 0.0
	F85	NA	NA
	W86	93.8 ± 12.4	62.0 ± 0.8
TM3	L104	0.0 ± 0.0	0.0 ± 0.0
	T105	2.3 ± 1.3	6.6 ± 1.0
	Y108	42.6 ± 1.0	9.6 ± 0.2
	F112	0.9 ± 3.0	9.1 ± 0.5
	F113	58.2 ± 8.7	18.1 ± 2.3
	F117	11.8 ± 2.0	5.4 ± 0.7
	F118	0.0 ± 0.0	0.0 ± 0.0
	L121	0.0 ± 0.0	0.0 ± 0.0
	L122	0.3 ± 0.6	0.0 ± 0.0
	T123	0.0 ± 0.0	0.0 ± 0.0
TM4	F144	1.5 ± 2.6	0.0 ± 0.0
TM5	T195	0.5 ± 1.4	0.0 ± 0.0
	I198	79.6 ± 6.7	72.2 ± 3.3
TM6	Y251	NA	NA
	N252	6.1 ± 1.4	11.1 ± 2.0
	L255	3.7 ± 1.5	2.8 ± 1.1
	N258	0.0 ± 0.0	0.0 ± 0.0
	T259	0.0 ± 0.0	0.0 ± 0.0
TM7	M279	0.0 ± 0.0	0.0 ± 0.0
	E283	118.7 ± 18.4	94.6 ± 13.3
	H289	0.5 ± 2.2	0.0 ± 0.0
	N293	NA	NA
	Y297	2.9 ± 2.8	0.0 ± 0.0

^aEntry of HIV-1_JR-FL Env-pseudotyped reporter viruses into U87-CD4 cells transiently expressing CCR5 alanine mutants was measured in the presence of 100 nM AD101 or SCH-C. Relative HIV-1 entry in the presence of inhibitors was calculated as (RLU with inhibitor/RLU without inhibitor) × 100%. All values are means ± SD of three independent experiments. NA = not applicable; alanine substitutions of residues Y68 and T82 in TM2, Y251 in TM6, and N293 in TM7 were excluded from the study because they are substantially defective at mediating HIV-1 entry (<1% of wild-type CCR5 coreceptor function) (13).

^bValues shown in bold are significantly higher than the cutoff level of inhibition (16%).