TABLE 1.

Anti-HIV activity of selected compounds against virus strains made resistant to entry inhibitors

Compound	EC50 (μM)a		EC50 (mM) (fold resistance)b
	HIV-1 NL4-3	AR177-resc	ADS-J1-res Ara49	ADS-J1-res Ara45C	BMS-res	AMD3100-res	T20/C34-res	SFV-res
ADS-J1	0.1 ± 0.04	2.04 ± 0.24	14.6 ± 2.4 (146)	12.3 ± 1.4 (123)	0.2 ± 0.002 (2)	1.7 ± 0.4 (17)	0.4 ± 0.16 (4)	0.08 ± 0.01(1)
BMS-155	0.02 ± 0.004	0.005 ± 0.004	0.1 ± 0.04 (5)	0.05 ± 0.01 (3)	>2.7 ± n.a. (>350)	0.03 ± 0.008 (2)	0.031 ± 0.004 (2)	0.007 ± 0.0007 (0)
AMD3100	0.002 ± 0.002	0.01 ± 0.006	0.003 ± 0.0006 (2)	0.006 ± 0.0005 (3)	0.004 ± 0.002 (2)	0.7 ± (350)	0.003 ± 0.002 (2)	0.002 ± 0.0008 (1)
Dextran sulfate	0.05 ± 0.01	0.37 ± 0.26	10.07 ± 7.12 (200)	17.2 ± 1.74 (344)	0.005 ± 0.002 (0)	>25 ± n.a. (>500)	0.05 ± 0.03 (1)	0.005 ± 0.003 (0)
C34	0.0002 ± 0.0003	0.0005 ± 0.0003	0.0007 ± 0.0006 (4)	0.001 ± 0.001 (5)	0.001 ± 0.0003 (5)	0.005 ± 0.0008 (25)	0.01 ± 0.003 (60)	0.15 ± 0.03 (750)
T20	0.09 ± 0.04	0.004 ± 0.004	0.5 ± 0.06 (5)	0.5 ± 0.49 (5)	0.2 ± 0.10 (3)	0.06 ± 0.01 (1)	>2.5 ± n.a. (>20)	0.9 ± 0.01 (10)
Sifuvirtide	0.001 ± 0.00005	0.0004 ± 0.0005	0.002 ± 0.003 (2)	0.002 ± 0.002 (2)	0.002 ± 0.001 (2)	0.008 ± 0.001 (4)	0.01 ± 0.01 (10)	1.03 ± 0.04 (>1,000)
AZT	0.007 ± 0.004	0.007 ± 0.008	0.015 ± 0.01 (2)	0.01 ± 0.007 (1)	0.01 ± 0.006 (1)	0.004 ± 0.005 (1)	0.007 ± 0.001 (1)	0.003 ± 0.0008 (0)

^aEC₅₀: 50% effective concentration, or the concentration needed to block replication of the wild-type NL4-3 HIV-1 in MT-4 cells.

^bFold change in EC₅₀ compared to that of the wild-type HIV-1 NL4-3 strain. Data represent the means and standard deviations of results of at least two independent evaluations done in triplicate. n.a., not available.

^cres, HIV-1 strain resistant to the corresponding drug.