Cloned (Comment) | Organism |
---|---|
- |
Human immunodeficiency virus 1 |
Protein Variants | Comment | Organism |
---|---|---|
V32I | under drug pressure commonly selected mutant | Human immunodeficiency virus 1 |
V82A | under drug pressure commonly selected mutant | Human immunodeficiency virus 1 |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(3S,4aS,8aS)-2-((2R,3S)-4-(benzo[b]thiophen-2-yl)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)butyl)-N-tert-butyldecahydroisoquinoline-3-carboxamide | - |
Human immunodeficiency virus 1 | |
(3S,4aS,8aS)-N-tert-butyl-2-((2R,3R)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)-3-(4-phenylthiophen-2-yl)propyl)decahydroisoquinoline-3-carboxamide | - |
Human immunodeficiency virus 1 | |
(3S,4aS,8aS)-N-tert-butyl-2-((2R,3S)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)-4-(4-phenylthiophen-2-yl)butyl)decahydroisoquinoline-3-carboxamide | - |
Human immunodeficiency virus 1 | |
(3S,4aS,8aS)-N-tert-butyl-2-((2R,3S)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)-4-(thiophen-2-yl)butyl)decahydroisoquinoline-3-carboxamide | - |
Human immunodeficiency virus 1 | |
(3S,4aS,8aS)-N-tert-butyl-2-[(2R,3S)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(thiophen-2-yl)butyl]decahydroisoquinoline-3-carboxamide | - |
Human immunodeficiency virus 1 | |
(R)-N1-((1R,2R)-3-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2-(1H)-yl)-2-hydroxy-1-(4-phenylthiophen-2-yl)propyl)-2-(quinoline-2-carboxamido)succinamide | - |
Human immunodeficiency virus 1 | |
(R)-N1-((2S,3R)-1-(benzo[b]thiophen-2-yl)-4-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl)-3-hydroxybutan-2-yl)-2-(quinoline-2-carboxamido)succinamide | - |
Human immunodeficiency virus 1 | |
(R)-N1-((2S,3R)-4-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl)-2-hydroxy-1-(thiophen-2-yl)propyl)-2-(quinoline-2-carboxamido)succinamide | - |
Human immunodeficiency virus 1 | |
(R)-N1-((2S,3R)-4-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl)-3-hydroxy-1-(4-phenylthiophen-2-yl)butan-2-yl)-2-(quinoline-2-carboxamido)succinamide | - |
Human immunodeficiency virus 1 | |
(R)-N1-((2S,3R)-4-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl)-3-hydroxy-1-(thiophen-2-yl)butan-2-yl)-2-(quinoline-2-carboxamido)succinamide | - |
Human immunodeficiency virus 1 | |
nelfinavir | - |
Human immunodeficiency virus 1 | |
saquinavir | - |
Human immunodeficiency virus 1 |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Human immunodeficiency virus 1 | - |
- |
- |
Purification (Comment) | Organism |
---|---|
- |
Human immunodeficiency virus 1 |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
Abz-Thr-Ile-Nle-Phe(NO2)-Gln-Arg + H2O | - |
Human immunodeficiency virus 1 | Abz-Thr-Ile-Nle + Phe(NO2)-Gln-Arg | - |
? |
Synonyms | Comment | Organism |
---|---|---|
HIV-1 protease | - |
Human immunodeficiency virus 1 |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0000004 | - |
- |
Human immunodeficiency virus 1 | saquinavir | |
0.0000006 | - |
wild-type protein, with 1 nM: 53% residual activity of wild-type protein, 54% residual activity of V32I mutant protein and 37% residual activity of V82A mutant protein | Human immunodeficiency virus 1 | (R)-N1-((2S,3R)-1-(benzo[b]thiophen-2-yl)-4-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl)-3-hydroxybutan-2-yl)-2-(quinoline-2-carboxamido)succinamide | |
0.0000012 | - |
- |
Human immunodeficiency virus 1 | (R)-N1-((2S,3R)-4-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl)-3-hydroxy-1-(4-phenylthiophen-2-yl)butan-2-yl)-2-(quinoline-2-carboxamido)succinamide | |
0.0000019 | - |
- |
Human immunodeficiency virus 1 | nelfinavir | |
0.0000029 | - |
wild-type protein, with 1 nM: 34% residual activity of wild-type protein, 97% residual activity of V32I mutant protein and 60% residual activity of V82A mutant protein, with 10 nM: 5% residual activity of wild-type protein and 32% residual activity of V32I mutant protein | Human immunodeficiency virus 1 | (3S,4aS,8aS)-N-tert-butyl-2-((2R,3S)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)-4-(thiophen-2-yl)butyl)decahydroisoquinoline-3-carboxamide | |
0.000006 | - |
- |
Human immunodeficiency virus 1 | (3S,4aS,8aS)-N-tert-butyl-2-((2R,3S)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)-4-(4-phenylthiophen-2-yl)butyl)decahydroisoquinoline-3-carboxamide | |
0.000015 | - |
- |
Human immunodeficiency virus 1 | (3S,4aS,8aS)-2-((2R,3S)-4-(benzo[b]thiophen-2-yl)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)butyl)-N-tert-butyldecahydroisoquinoline-3-carboxamide | |
0.000021 | - |
- |
Human immunodeficiency virus 1 | (R)-N1-((2S,3R)-4-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl)-3-hydroxy-1-(thiophen-2-yl)butan-2-yl)-2-(quinoline-2-carboxamido)succinamide | |
0.0015 | - |
- |
Human immunodeficiency virus 1 | (R)-N1-((1R,2R)-3-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2-(1H)-yl)-2-hydroxy-1-(4-phenylthiophen-2-yl)propyl)-2-(quinoline-2-carboxamido)succinamide | |
0.004 | - |
- |
Human immunodeficiency virus 1 | (3S,4aS,8aS)-N-tert-butyl-2-((2R,3R)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)-3-(4-phenylthiophen-2-yl)propyl)decahydroisoquinoline-3-carboxamide | |
0.005 | - |
- |
Human immunodeficiency virus 1 | (R)-N1-((2S,3R)-4-((3S,4aS,8aS)-3-(tert-butylcarbamoyl)octahydroisoquinolin-2(1H)-yl)-2-hydroxy-1-(thiophen-2-yl)propyl)-2-(quinoline-2-carboxamido)succinamide | |
0.03 | - |
- |
Human immunodeficiency virus 1 | (3S,4aS,8aS)-N-tert-butyl-2-[(2R,3S)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(thiophen-2-yl)butyl]decahydroisoquinoline-3-carboxamide |