Table 2 Compounds targeting binding site 1: FG binding site

PF74 [137]

N53, L56, N57, V59, Q63, M66, Q67, L69, K70, I73, A105, T107, Y130

Stabilize, increase multimerization

Early/late

0.57 µM

69 µM

13m [149]

N/A

N/A

N/A

4.33 µM

57.7 µM

II-10C [153]

C14, I15, P17, L20, N21, Q50, T54, N57, T58, G60, K70^b

N/A

N/A

2.13 µM

35.5 µM

11I [154]

Q50, N53, T54, L56, N57, K70, N74, G106^b

Decrease multimerization

Early/late

0.09 µM

34.5 µM

6a-9 [155]

N53, L56, N57, M66, K70, I73, N74, A105, T107^b

No effect on multimerization

Early/late

3.13 µM

16.5 µM

H22 [156]

L56, N57, Q63, M66, L69, K70, I73, Y130, Y169, L172, R173, K182^b

Increase multimerization

N/A

18.1 µM^a

526 µM

CX06 [150]

N/A

Destabilize, decrease multimerization

Early/late

5.9 µM^a

> 100 µM

10 [157]

P34, N53, L56, N57, L59, Q63, M66, K70, Y130, R173, Q179, K182^b

Stabilize

N/A

1.6 µM

> 100 µM

12 [158]

N53, N57, Q63, K70, N74, G106, Y130, R173, Q179, K182^b

Stabilize

N/A

0.032 µM

 > 100 µM

15 [159]

N57, Q63, K70, T107, K182^b

Stabilize

N/A

0.31 µM

44 µM

20 [151]

N53, N57, Q63, K70, G106, T107, Y130, R173, Q179, K182^b

Stabilize

N/A

0.88 µM

> 50 µM

32 [152]

N53, N57, Q63, Q67, KN74, K70, Y130, Y169, R173, Q179, K182^b

Stabilize

N/A

0.14 µM

45 µM

58 [152]

Stabilize

N/A

0.15 µM

14 µM

BI-1 [160]

N53, L56, N57, M66, L69, K70, I73, N74, A105, G106, T107, Y130

Stabilize, increase multimerization

Early/late

8.2 µM

> 92 µM

BI-2 [160]

Stabilize, increase multimerization

Early/late

1.8 µM

> 43 µM

BMMP [173]

N/A

Decrease multimerization

Late

25 µM^a

N/A

C-A1 [174, 175]

Q50, N53, N57, N63, Q67, N70, N74, A105, T107, N112, E128, R173, Q179, K182^b

N/A

Early

0.98 µM^a

8.0 µM

GS-CA1 [162]

L57, N57, M66, Q67, K70, N74, T107^b

Increase multimerization

Early/late

240 pM

N/A

GS-6207 [135]

N57, K70, N74, N183

Increase multimerization

Early/late

95 pM

> 50 µM

ViiV-1 [170,171,172]

N/A

N/A

Early

25 pM

N/A