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Literature summary for 3.1.26.13 extracted from
- Small molecule inhibitors of HIV RT Ribonuclease H (2010), Bioorg. Med. Chem. Lett., 20, 398-402.
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2-oxo-2-[(2,3,4-trichlorophenyl)amino]ethyl benzyl(phenyl)carbamodithioate | - |
Human immunodeficiency virus 1 |  |
| 2-oxo-2-[(2,3,4-trichlorophenyl)amino]ethyl dibenzylcarbamodithioate | - |
Human immunodeficiency virus 1 | |
| 2-[(2,3,4-trichlorophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate | inhibitor indentified by FRET-based high-throughput screening assay | Human immunodeficiency virus 1 | |
| 2-[(2,4-dichlorophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate | - |
Human immunodeficiency virus 1 | |
| 2-[(2,4-dimethylphenyl)amino]-2-oxoethyl dibenzylcarbamodithioate | inhibitor indentified by FRET-based high-throughput screening assay | Human immunodeficiency virus 1 | |
| 2-[(2-methoxy-5-methylphenyl)amino]-2-oxoethyl benzyl(phenyl)carbamodithioate | - |
Human immunodeficiency virus 1 | |
| 2-[(3-cyanophenyl)amino]-2-oxoethyl benzyl(phenyl)carbamodithioate | - |
Human immunodeficiency virus 1 | |
| 2-[(3-cyanophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate | - |
Human immunodeficiency virus 1 | |
| 2-[4-benzyl-5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]pyridine | inhibitor indentified by FRET-based high-throughput screening assay | Human immunodeficiency virus 1 | |
| 2-[4-benzyl-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridine | - |
Human immunodeficiency virus 1 | |
| 3-(furan-2-yl)-4-(4-methoxybenzyl)-5-[[4-(trifluoromethyl)benzyl]sulfanyl]-4H-1,2,4-triazole | - |
Human immunodeficiency virus 1 | |
| 3-(furan-2-yl)-4-phenyl-5-[[4-(trifluoromethyl)benzyl]sulfanyl]-4H-1,2,4-triazole | - |
Human immunodeficiency virus 1 | |
| 4-([[4-benzyl-5-(furan-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine | - |
Human immunodeficiency virus 1 | |
| 4-([[4-benzyl-5-(thiophen-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine | inhibitor indentified by FRET-based high-throughput screening assay | Human immunodeficiency virus 1 | |
| 4-benzyl-3-(benzylsulfanyl)-5-(furan-2-yl)-4H-1,2,4-triazole | inhibitor indentified by FRET-based high-throughput screening assay | Human immunodeficiency virus 1 | |
| 4-benzyl-3-(benzylsulfanyl)-5-(thiophen-2-yl)-4H-1,2,4-triazole | inhibitor indentified by FRET-based high-throughput screening assay | Human immunodeficiency virus 1 | |
| 4-benzyl-3-(benzylsulfanyl)-5-phenyl-4H-1,2,4-triazole | inhibitor indentified by FRET-based high-throughput screening assay | Human immunodeficiency virus 1 | |
| 4-benzyl-3-(furan-2-yl)-5-[(4-methoxybenzyl)sulfanyl]-4H-1,2,4-triazole | - |
Human immunodeficiency virus 1 | |
| 4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-(furan-2-yl)-4H-1,2,4-triazole | - |
Human immunodeficiency virus 1 | |
| 4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole | inhibitor indentified by FRET-based high-throughput screening assay | Human immunodeficiency virus 1 | |
| 4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-phenyl-4H-1,2,4-triazole | - |
Human immunodeficiency virus 1 | |
| 4-benzyl-3-[(4-methoxybenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole | - |
Human immunodeficiency virus 1 | |
| 4-benzyl-3-[(4-methoxybenzyl)sulfanyl]-5-phenyl-4H-1,2,4-triazole | inhibitor indentified by FRET-based high-throughput screening assay | Human immunodeficiency virus 1 | |
| additional information | identification and evaluation of thiocarbamate and triazole inhibitors targeting RNase H activity of HIV reverse transcriptase, overview | Human immunodeficiency virus 1 |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Human immunodeficiency virus 1 | - |
- |
- |
| Human immunodeficiency virus 1 | - |
HIV-1 | - |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| ribonuclease H | - |
Human immunodeficiency virus 1 |
| RNase H | - |
Human immunodeficiency virus 1 |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0002 | - |
pH 8.0, 25°C | Human immunodeficiency virus 1 | 4-([[4-benzyl-5-(thiophen-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine | |
| 0.00021 | - |
pH 8.0, 25°C | Human immunodeficiency virus 1 | 4-benzyl-3-(benzylsulfanyl)-5-(thiophen-2-yl)-4H-1,2,4-triazole | |
| 0.00021 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 4-benzyl-3-(benzylsulfanyl)-5-(thiophen-2-yl)-4H-1,2,4-triazole | |
| 0.001 | - |
pH 8.0, 25°C | Human immunodeficiency virus 1 | 4-benzyl-3-(benzylsulfanyl)-5-phenyl-4H-1,2,4-triazole | |
| 0.001 | - |
pH 8.0, 25°C | Human immunodeficiency virus 1 | 4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole | |
| 0.001 | - |
pH 8.0, 25°C | Human immunodeficiency virus 1 | 4-benzyl-3-[(4-methoxybenzyl)sulfanyl]-5-phenyl-4H-1,2,4-triazole | |
| 0.001 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 4-benzyl-3-(benzylsulfanyl)-5-phenyl-4H-1,2,4-triazole | |
| 0.001 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole | |
| 0.001 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 4-benzyl-3-[(4-methoxybenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole | |
| 0.0012 | - |
pH 8.0, 25°C | Human immunodeficiency virus 1 | 4-benzyl-3-(benzylsulfanyl)-5-(furan-2-yl)-4H-1,2,4-triazole | |
| 0.0012 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 4-benzyl-3-(benzylsulfanyl)-5-(furan-2-yl)-4H-1,2,4-triazole | |
| 0.0017 | - |
pH 8.0, 25°C | Human immunodeficiency virus 1 | 2-[4-benzyl-5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]pyridine | |
| 0.0017 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 2-[4-benzyl-5-(benzylsulfanyl)-4H-1,2,4-triazol-3-yl]pyridine | |
| 0.0019 | - |
pH 8.0, 25°C | Human immunodeficiency virus 1 | 2-[(2,4-dimethylphenyl)amino]-2-oxoethyl dibenzylcarbamodithioate | |
| 0.0019 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 2-[(2,4-dimethylphenyl)amino]-2-oxoethyl dibenzylcarbamodithioate | |
| 0.0026 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 2-[4-benzyl-5-[(pyridin-4-ylmethyl)sulfanyl]-4H-1,2,4-triazol-3-yl]pyridine | |
| 0.0028 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-(furan-2-yl)-4H-1,2,4-triazole | |
| 0.0033 | - |
pH 8.0, 25°C | Human immunodeficiency virus 1 | 2-[(2,3,4-trichlorophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate | |
| 0.0033 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 2-oxo-2-[(2,3,4-trichlorophenyl)amino]ethyl dibenzylcarbamodithioate | |
| 0.0038 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 4-benzyl-3-(furan-2-yl)-5-[(4-methoxybenzyl)sulfanyl]-4H-1,2,4-triazole | |
| 0.004 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 4-([[4-benzyl-5-(furan-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine | |
| 0.0047 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 2-[(3-cyanophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate | |
| 0.0047 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 3-(furan-2-yl)-4-phenyl-5-[[4-(trifluoromethyl)benzyl]sulfanyl]-4H-1,2,4-triazole | |
| 0.0058 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 2-[(2,4-dichlorophenyl)amino]-2-oxoethyl dibenzylcarbamodithioate | |
| 0.0059 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 4-benzyl-3-[(4-methoxybenzyl)sulfanyl]-5-(thiophen-2-yl)-4H-1,2,4-triazole | |
| 0.006 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 4-benzyl-3-[(4-chlorobenzyl)sulfanyl]-5-phenyl-4H-1,2,4-triazole | |
| 0.0065 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 3-(furan-2-yl)-4-(4-methoxybenzyl)-5-[[4-(trifluoromethyl)benzyl]sulfanyl]-4H-1,2,4-triazole | |
| 0.0083 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 2-[(2-methoxy-5-methylphenyl)amino]-2-oxoethyl benzyl(phenyl)carbamodithioate | |
| 0.0114 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 2-[(3-cyanophenyl)amino]-2-oxoethyl benzyl(phenyl)carbamodithioate | |
| 0.0266 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 2-oxo-2-[(2,3,4-trichlorophenyl)amino]ethyl benzyl(phenyl)carbamodithioate | |
| 0.2 | - |
pH not specified in the publication, temperature not specified in the publication | Human immunodeficiency virus 1 | 4-([[4-benzyl-5-(thiophen-2-yl)-4H-1,2,4-triazol-3-yl]sulfanyl]methyl)pyridine | |
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