. Author manuscript; available in PMC: 2009 Sep 12.

Published in final edited form as: J Mol Biol. 2008 Jun 20;381(4):956–974. doi: 10.1016/j.jmb.2008.06.041

TABLE 1.

Anti-HIV activity against wt-R5-HIV-1 and binding affinity to wt-CCR5 of CCR5 inhibitors

		Antiviral assay (Virus) [IC₅₀^a and IC ₉₀, nM]			Binding Assay (K_D, nM)

Compound		MAGI with HIV-1_JRFL	MAGI with HIV-1_Ba-L	PHA-PBM with HIV-1_Ba-L

AK530	IC₅₀	2.8 ± 1.5^b	2.1 ± 1.1	32 ± 27	1.4 ± 0.9
AK530	IC₉₀	51 ± 2.5	79 ± 34	430 ± 113	1.4 ± 0.9
AK317	IC₅₀	2.0 ± 0.2	1.5 ± 1.9	25 ± 8	16.7 ± 7.5
AK317	IC₉₀	19 ± 14	25 ± 3	171 ± 45	16.7 ± 7.5
APL	IC₅₀	0.2 ± 0.1	0.2 ± 0.1	0.7 ± 0.4	3.6 ± 1.4
APL	IC₉₀	1.8 ± 0.7	2.9 ± 1.6	12 ± 10	3.6 ± 1.4

The IC₅₀ values were determined with the MAGI assay and the PHA-PBM (p24) assay (see "Materials and Methods").

The numbers denote the IC₅₀, IC₉₀ or K_D values (mean ± 1 S.D.).