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Literature summary for 2.3.1.286 extracted from
- Development and characterization of 3-(benzylsulfonamido)benzamides as potent and selective SIRT2 inhibitors (2014), Eur. J. Med. Chem., 76, 414-426.
Application
| Application | Comment | Organism |
|---|---|---|
| medicine | inhibitors of sirtuin-2 deacetylase are protective in various models of Huntingtons disease by decreasing polyglutamine aggregation, a hallmark of pathology of Huntingtons disease | Homo sapiens |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 2-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyano-2-fluorophenyl)isonicotinamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 | Homo sapiens |  |
| 2-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyanophenyl)isonicotinamide | selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 | Homo sapiens | |
| 3-(azepan-1-ylsulfonyl)-N-(3-nitrophenyl)benzamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 | Homo sapiens | |
| 3-(N-(4-acetylphenyl)-N-methylsulfamoyl)-N-(4-chlorophenyl)benzamide | highly selective inhibitor for SIRT2, no inhibition of SIRT1, low inhibition of and SIRT3 | Homo sapiens | |
| 3-(N-(4-acetylphenyl)-N-methylsulfamoyl)-N-(4-cyanophenyl)benzamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 | Homo sapiens | |
| 3-(N-(4-acetylphenyl)-N-methylsulfamoyl)-N-(5-chloropyridin-2-yl)benzamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3 | Homo sapiens | |
| 3-(N-(4-bromophenyl)-N-methylsulfamoyl)-N-(4-chloro-2-fluorophenyl)-N-methylbenzamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 | Homo sapiens | |
| 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-(methylsulfinyl)phenyl)benzamide | highly selective inhibitor for SIRT2, no inhibition of SIRT1, low inhibition of and SIRT3 | Homo sapiens | |
| 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-(methylsulfonyl)phenyl)benzamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 | Homo sapiens | |
| 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyano-2-fluorophenyl)benzamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 | Homo sapiens | |
| 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyanophenyl)benzamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3 | Homo sapiens | |
| 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(5-cyanopyridin-2-yl)benzamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3 | Homo sapiens | |
| 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(5-fluoropyridin-2-yl)benzamide | highly selective inhibitor for SIRT2, no inhibition of SIRT1 and SIRT3 | Homo sapiens | |
| 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(6-chloropyridazin-3-yl)benzamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1 | Homo sapiens | |
| 3-(N-(5-chloropyridin-2-yl)-N-methylsulfamoyl)-N-(4-cyanophenyl)benzamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 | Homo sapiens | |
| 4-bromo-N-(3-(N-methyl-N-(4-(methylsulfonyl)phenyl)sulfamoyl)phenyl)benzamide | selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 | Homo sapiens | |
| N-(3-(N-(4-chlorophenyl)-N-methylsulfamoyl)phenyl)-4-cyanobenzamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3 | Homo sapiens | |
| N-(4-acetylphenyl)-3-(N-(4-acetylphenyl)-N-methylsulfamoyl)benzamide | highly selective inhibitor for SIRT2, no inhibition of SIRT1 and SIRT3 | Homo sapiens | |
| N-(4-bromo-2-fluorophenyl)-3-(N-(4-bromophenyl)-N-methylsulfamoyl)-N-methylbenzamide | highly selective inhibitor for SIRT2, no inhibition of SIRT1 and SIRT3 | Homo sapiens | |
| N-(4-chlorophenyl)-3-(N-methyl-N-(4-(methylsulfonyl)phenyl)sulfamoyl)benzamide | highly selective inhibitor for SIRT2, no inhibition of SIRT1 and SIRT3 | Homo sapiens | |
| N-(4-cyanophenyl)-3-(N-(4-(1-hydroxyethyl)phenyl)-N-methylsulfamoyl)benzamide | - |
Homo sapiens | |
| N-(4-cyanophenyl)-3-(N-(4-fluorophenyl)-N-methylsulfamoyl)benzamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 | Homo sapiens | |
| N-(4-cyanophenyl)-3-(N-(4-methoxyphenyl)-N-methylsulfamoyl)benzamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1 and SIRT3 | Homo sapiens | |
| N-(4-cyanophenyl)-3-(N-methyl-N-(4-(methylsulfonyl)phenyl)sulfamoyl)benzamide | highly selective inhibitor for SIRT2, low inhibition of SIRT1, no inhibition of and SIRT3 | Homo sapiens | |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | Q8IXJ6 | - |
- |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| NAD+ + [alpha-tubulin]-N6-acetyl-L-lysine40 | - |
Homo sapiens | nicotinamide + [alpha-tubulin]-L-lysine40 + 2'-O-acetyl-ADP ribose | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| SIRT2 | - |
Homo sapiens |
| sirtuin-2 deacetylase | - |
Homo sapiens |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.0038 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(3-(N-(4-chlorophenyl)-N-methylsulfamoyl)phenyl)-4-cyanobenzamide | |
| 0.0049 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyanophenyl)isonicotinamide | |
| 0.0061 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyanophenyl)benzamide | |
| 0.0061 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(N-(5-chloropyridin-2-yl)-N-methylsulfamoyl)-N-(4-cyanophenyl)benzamide | |
| 0.0063 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-bromo-N-(3-(N-methyl-N-(4-(methylsulfonyl)phenyl)sulfamoyl)phenyl)benzamide | |
| 0.0066 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyano-2-fluorophenyl)benzamide | |
| 0.0068 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(N-(4-acetylphenyl)-N-methylsulfamoyl)-N-(4-chlorophenyl)benzamide | |
| 0.0069 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-bromo-2-fluorophenyl)-3-(N-(4-bromophenyl)-N-methylsulfamoyl)-N-methylbenzamide | |
| 0.0073 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(N-(4-acetylphenyl)-N-methylsulfamoyl)-N-(4-cyanophenyl)benzamide | |
| 0.0075 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(N-(4-bromophenyl)-N-methylsulfamoyl)-N-(4-chloro-2-fluorophenyl)-N-methylbenzamide | |
| 0.0091 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(5-fluoropyridin-2-yl)benzamide | |
| 0.0094 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-cyanophenyl)-3-(N-(4-fluorophenyl)-N-methylsulfamoyl)benzamide | |
| 0.0095 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-(methylsulfinyl)phenyl)benzamide | |
| 0.0095 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-cyanophenyl)-3-(N-methyl-N-(4-(methylsulfonyl)phenyl)sulfamoyl)benzamide | |
| 0.0096 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-cyanophenyl)-3-(N-(4-methoxyphenyl)-N-methylsulfamoyl)benzamide | |
| 0.0098 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-(methylsulfonyl)phenyl)benzamide | |
| 0.0102 | - |
pH and temperature not specified in the publication | Homo sapiens | 2-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(4-cyano-2-fluorophenyl)isonicotinamide | |
| 0.0108 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(azepan-1-ylsulfonyl)-N-(3-nitrophenyl)benzamide | |
| 0.0115 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-cyanophenyl)-3-(N-(4-(1-hydroxyethyl)phenyl)-N-methylsulfamoyl)benzamide | |
| 0.0132 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(N-(4-acetylphenyl)-N-methylsulfamoyl)-N-(5-chloropyridin-2-yl)benzamide | |
| 0.0156 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(6-chloropyridazin-3-yl)benzamide | |
| 0.0159 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-chlorophenyl)-3-(N-methyl-N-(4-(methylsulfonyl)phenyl)sulfamoyl)benzamide | |
| 0.0189 | - |
pH and temperature not specified in the publication | Homo sapiens | N-(4-acetylphenyl)-3-(N-(4-acetylphenyl)-N-methylsulfamoyl)benzamide | |
| 0.0199 | - |
pH and temperature not specified in the publication | Homo sapiens | 3-(N-(4-chlorophenyl)-N-methylsulfamoyl)-N-(5-cyanopyridin-2-yl)benzamide | |
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