Table 3 Activity of CCR5 inhibitors against HIV-1s, including MVC-resistant HIV-1.

From: Activity and structural analysis of GRL-117C: a novel small molecule CCR5 inhibitor active against R5-tropic HIV-1s

Virus

IC50 [IC90] values (nM)a

MVC

CVC

GRL-117C

YU2b

3.5 ± 2.5 [15 ± 15]

1.1 ± 0.7 [6.2 ± 5.7]

68 ± 8.8 [>100]

KP-5pcb

8.5 ± 3.6 [81 ± 41]

4.9 ± 2.2 [105 ± 62]

160 ± 30 [767 ± 26]

KP-5mvcRc

36 ± 28 [236 ± 146]

260 ± 352 [>300]

686 ± 89 [>100]

  1. aIC50 [IC90] numbers were obtained via the TZM-bl assay. Data are expressed as mean ± SD.
  2. bDrug-sensitive HIV-1 strains.
  3. cMVC-resistant HIV-1 strain.
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