TABLE 7.

Sensitivity of mutant HIV-1(III_B) strains towards various HIV-1 RT inhibitors

Compound	EC50 (μg/ml)a
	Wild type	Tyr181Cys (JPL-71)c	Lys103Asn (JPL-71)c	Glu138Lys (JPL-74)c	Tyr188His (JPL-71)c	Val179Asp (JPL-107)c	Leu100Ile
Nevirapine	0.006 ± 0.001	2.2 ± 0.9	1.8 ± 0.5	0.04 ± 0.02	0.02 ± 0.002	0.02 ± 0.001	0.06 ± 0.02
Efavirenz	0.0006 ± 0.0001	0.003 ± 0.001	0.02 ± 0.001	0.003 ± 0.001	0.002 ± 0.001	0.002 ± 0.001	0.01 ± 0.007
UC-781	0.002 ± 0.001	0.06 ± 0.02	0.07 ± 0.04	0.007 ± 0.004	0.012 ± 0.001	0.003 ± 0.001	0.02 ± 0.008
AZT	0.002 ± 0.0008	0.001 ± 0.0003	0.005 ± 0.001	0.003 ± 0.0008	0.001 ± 0.0003	0.001 ± 0.0003	0.002 ± 0.0005
3TC	0.03 ± 0.02	0.02 ± 0.001	0.03 ± 0.008	0.02 ± 0.004	0.01 ± 0.004	0.02 ± 0.003	0.03 ± 0.006
Tenofovir	1.0 ± 0.8	1.1 ± 0.4	1.7 ± 0.2	1.2 ± 0.5	0.8 ± 0.6	0.9 ± 0.6	1.1 ± 0.4
JPL-10	5.3 ± 2.6	20 ± 6	11 ± 5	12 ± 4	8.8 ± 1.1	8.0 ± 0.1	10 ± 2
JPL-27	6.8 ± 3.5	>20	16 ± 6	≥20			≥20
JPL-30	5.9 ± 3.0	50 ± 4	44 ± 4	48 ± 24			40 ± 8
JPL-71	0.10 ± 0.01	≥20	12 ± 1	4 ± 3	8.8 ± 1.1	0.35 ± 0.09	4.6 ± 2.1
JPL-74	0.48 ± 0.01	>4b	>4b	>4b			>4b
JPL-78	3.4 ± 0.9	50 ± 23	50 ± 25	60 ± 22			60 ± 26
JPL-107	0.52 ± 0.03	>4b	>4b	>4b	2.4 ± 0.4	>4b	>4b
JPL-110	9.6 ± 1.4	60 ± 25	48 ± 24	60 ± 4			50 ± 21
JPL-133	0.05 ± 0.01	≥20	4.8 ± 1.9	1.2 ± 0.8	9.2 ± 1.7	0.32 ± 0.04	0.2 ± 0.1
JPL-146	2.2 ± 0.2	≥20	9.6 ± 1.1	≥20			1.9 ± 0.7
JPL-150	4.0 ± 0.1	>20	>20	>20			10 ± 1

^aEC₅₀, compound concentration required to inhibit HIV-1-induced cytopathicity (giant cell formation) in CEM cell cultures. Data represent the average values (± SD) for at least three independent experiments.

^bHigher drug concentrations could not be accurately determined due to insolubility of the compound at these concentrations.

^cHIV-1 strain that emerged upon exposure to the pyridine oxide derivative indicated in parentheses.