Skip to main content

Table 4 Compounds targeting binding site 3: twofold binding site

From: Rotten to the core: antivirals targeting the HIV-1 capsid core

Name

Main Interactions

Effects on stability and/or assembly

HIV-1 Stage affected

IC50a/EC50

CC50

CAI [184]

Helix α1: 161–174

Helix α2: 180–192

Decrease multimerization

Early/late

N/A

N/A

NYAD-1 [185]

Helix α1: 161–174

Helix α2: 180–192

Decrease multimerization

N/A

4.0–15 µMa

57–80 µM

NYAD-13 [185]

I153, R154, Y164, A174, A177, V181, K182, A184, A194, I201, A204, G206, A209, E213, A217, Q219, V221, A228, V230

N/A

N/A

10.5 µMa

40.5 µM

CAC1 [188]

Helix α2b

N/A

N/A

N/A

N/A

NYAD-201 [190]

178–192b

Decrease multimerization

Early/late

2.8–5.2 µMa

> 115 µM

MKN-1A [191]

W184, M185b

N/A

N/A

8.0 µM

38 µM

16 [192]

N/A

N/A

N/A

5.0 µMa

N/A

Ebselen [193]

Helix α10: C198

Helix α11: C218

Decrease multimerization

Early

4.3 µM

37.9 µM

I-XW-053 [194]

R173, Ile37b

N/A

Early

48.4–93.6 µMa

> 100 µM

  1. Compound stabilizing effects on HIV-1 CA were determined by thermal shift assays and compounds effects on capsid assembly were determined by in vitro capsid assembly assays
  2. N/A not available
  3. aRefers to IC50
  4. bRefers to key interactions found through non-structural studies such as molecular docking