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

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

Virus

IC50 [IC90] (nM)

MVC

SCH-C

APL

TAK-779

GRL-117C

GRL-10007C

GRL-10018C

Ba-L (MAGI)a

0.7 [6.4]

4.8 [15.9]

0.2 [4.9]

15.7 [88.1]

0.6 [8.9]

1.4 [9.5]

2.9 [27.5]

Ba-L (PBMCs)b

4.5 [21.6]

13.9 [97.2]

2.6 [13.4]

31.6 [187]

8.1 [48.3]

16.9 [126.5]

18.7 [154.7]

CC1/85 cl.6c

1.7 [n.d.d]

5.2 [n.d.d]

1.5 [n.d.d]

22.7 [n.d.d]

n.d.d [n.d.d]

12.5 [n.d.d]

n.d.d [n.d.d]

CC1/85 cl.7c

2.5 [20.6]

6.1 [67.7]

1.8 [11.3]

28.3 [101]

3.5 [28.9]

15.8 [80.3]

4.9 [34.9]

CC101.19 cl.7

36.9 [486]

>1000 [>1000]

16.3 [200]

400 [>1000]

32.5 [296]

41.1 [472]

52.5 [553]

(AD101 resistant)

(×15)e

(>×164)

(×9.1)

(×14)

(×9.3)

(×2.6)

(×11)

D1/85.16 cl.23

26.5 [376]

412 [>1000]

8.6 [98.6]

166 [747]

29.8 [415]

56.9 [536]

61.3 [642]

(VVC resistant)

(×11)e

(×68)

(×4.7)

(×5.9)

(×8.5)

(×3.6)

(×12.5)

  1. aIC50/[IC90] numbers were obtained by MAGI assay using MAGI cells and R5-HIV-1BaL.
  2. bIC50/[IC90] numbers were obtained by p24 assay using PBMCs and R5-HIV-1BaL.
  3. cDrug naïve R5-HIV-1 clinical strains.
  4. dnot done.
  5. eParentheses indicate fold increases of IC50s compared to wild type (CC1/85 cl.7).
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