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Literature summary for 3.4.21.76 extracted from

  • Hwang, T.L.; Wang, W.H.; Wang, T.Y.; Yu, H.P.; Hsieh, P.W.
    Synthesis and pharmacological characterization of 2-aminobenzaldehyde oxime analogs as dual inhibitors of neutrophil elastase and proteinase 3 (2015), Bioorg. Med. Chem., 23, 1123-1134.
    View publication on PubMed
Search for more literature for 3.4.21.76

Application

Application Comment Organism
drug development enzyme inhibitors may prove to be targets for the generation of agents in the treatment of neutrophilic inflammatory disease Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(E)-4-(N-(2-(1-(hydroxyimino)butyl)phenyl)sulfamoyl)phenyl pivalate
-
 Homo sapiens
(E)-4-(N-(2-(1-(hydroxyimino)ethyl)phenyl)sulfamoyl)phenyl pivalate the compound has several beneficial effects in inflammatory disease and lipopolysacchride-induced edema, overview Homo sapiens
(E)-4-(N-(2-(1-(hydroxyimino)methyl)phenyl)sulfamoyl)phenyl pivalate
-
 Homo sapiens
(E)-4-(N-(2-(1-(hydroxyimino)propyl)phenyl)sulfamoyl)phenyl pivalate
-
 Homo sapiens
(E)-4-(N-(2-(1-(methoxyimino)ethyl)phenyl)sulfamoyl)phenyl pivalate
-
 Homo sapiens
(Z)-4-(N-(2-(1-(methoxyimino)ethyl)phenyl)sulfamoyl)phenyl pivalate
-
 Homo sapiens
2-hydroxyethyl 2-(4-(pivaloyloxy)phenylsulfonamido)benzoate
-
 Homo sapiens
4-(N-(2-(2-hydroxyethylcarbamoyl)phenyl)sulfamoyl)phenyl pivalate
-
 Homo sapiens
4-(N-(2-acetylphenyl)sulfamoyl)phenyl 2-methylpropane-2-sulfinate
-
 Homo sapiens
4-(N-(2-acetylphenyl)sulfamoyl)phenyl pivalate
-
 Homo sapiens
4-(N-(2-butyrylphenyl)sulfamoyl)phenyl pivalate
-
 Homo sapiens
4-(N-(2-formylphenyl)sulfamoyl)phenyl 2-methylpropane-2-sulfinate
-
 Homo sapiens
4-(N-(2-formylphenyl)sulfamoyl)phenyl pivalate
-
 Homo sapiens
4-(N-(2-pentanoyl phenyl)sulfamoyl)phenyl pivalate
-
 Homo sapiens
4-(N-(2-propionylphenyl)sulfamoyl)phenyl pivalate
-
 Homo sapiens
ethyl 2-(4-(3,3,3-trifluoro-2,2-dimethylpropanoyloxy)benzamido)benzoate
-
 Homo sapiens
ethyl 2-(4-(pivaloyloxy)benzamido)benzoate
-
 Homo sapiens
methyl 2-(4-(3,3,3-trifluoro-2,2-dimethylpropanoyloxy)benzamido)benzoate
-
 Homo sapiens
methyl 2-(4-(3,3,3-trifluoro-2,2-dimethylpropanoyloxy)phenylsulfonamide)benzoate
-
 Homo sapiens
methyl 2-(4-(pivaloyloxy)benzamido)benzoate
-
 Homo sapiens
methyl 2-(4-pivalamidophenylsulfonamido)benzoate
-
 Homo sapiens
additional information synthesis and pharmacological characterization of 2-aminobenzaldehyde oxime analogues as dual inhibitors of neutrophil elastase and proteinase 3, structure–activity relationship analysis, overview Homo sapiens
propyl 2-(4-(3,3,3-trifluoro-2,2-dimethylpropanoyloxy)benzamido)benzoate
-
 Homo sapiens
propyl 2-(4-(pivaloyloxy)benzamido)benzoate
-
 Homo sapiens
sivelestat
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
azurophil granule a major neutrophilic serine protease expressed in neutrophil azurophil granules Homo sapiens 42582
-

Organism

Organism UniProt Comment Textmining
Homo sapiens P24158
-
-

Source Tissue

Source Tissue Comment Organism Textmining
neutrophil
-
 Homo sapiens
-

Synonyms

Synonyms Comment Organism
PR3
-
 Homo sapiens
proteinase 3
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00022
-
 pH 7.4, 30°C Homo sapiens (E)-4-(N-(2-(1-(hydroxyimino)ethyl)phenyl)sulfamoyl)phenyl pivalate
0.00031
-
 pH 7.4, 30°C Homo sapiens 4-(N-(2-(2-hydroxyethylcarbamoyl)phenyl)sulfamoyl)phenyl pivalate
0.00034
-
 pH 7.4, 30°C Homo sapiens sivelestat
0.00036
-
 pH 7.4, 30°C Homo sapiens 4-(N-(2-butyrylphenyl)sulfamoyl)phenyl pivalate
0.00047
-
 pH 7.4, 30°C Homo sapiens 4-(N-(2-acetylphenyl)sulfamoyl)phenyl pivalate
0.00053
-
 pH 7.4, 30°C Homo sapiens (E)-4-(N-(2-(1-(hydroxyimino)methyl)phenyl)sulfamoyl)phenyl pivalate
0.00061
-
 pH 7.4, 30°C Homo sapiens (E)-4-(N-(2-(1-(methoxyimino)ethyl)phenyl)sulfamoyl)phenyl pivalate
0.00061
-
 pH 7.4, 30°C Homo sapiens 2-hydroxyethyl 2-(4-(pivaloyloxy)phenylsulfonamido)benzoate
0.00109
-
 pH 7.4, 30°C Homo sapiens 4-(N-(2-propionylphenyl)sulfamoyl)phenyl pivalate
0.00173
-
 pH 7.4, 30°C Homo sapiens (E)-4-(N-(2-(1-(hydroxyimino)butyl)phenyl)sulfamoyl)phenyl pivalate
0.00205
-
 pH 7.4, 30°C Homo sapiens 4-(N-(2-formylphenyl)sulfamoyl)phenyl pivalate
0.00205
-
 pH 7.4, 30°C Homo sapiens methyl 2-(4-(pivaloyloxy)benzamido)benzoate
0.00231
-
 pH 7.4, 30°C Homo sapiens 4-(N-(2-pentanoyl phenyl)sulfamoyl)phenyl pivalate
0.00237
-
 pH 7.4, 30°C Homo sapiens (Z)-4-(N-(2-(1-(methoxyimino)ethyl)phenyl)sulfamoyl)phenyl pivalate
0.0025
-
 pH 7.4, 30°C Homo sapiens (E)-4-(N-(2-(1-(hydroxyimino)propyl)phenyl)sulfamoyl)phenyl pivalate
0.00302
-
 pH 7.4, 30°C Homo sapiens ethyl 2-(4-(pivaloyloxy)benzamido)benzoate
0.00391
-
 pH 7.4, 30°C Homo sapiens propyl 2-(4-(pivaloyloxy)benzamido)benzoate
0.00494
-
 pH 7.4, 30°C Homo sapiens methyl 2-(4-(3,3,3-trifluoro-2,2-dimethylpropanoyloxy)phenylsulfonamide)benzoate
0.01
-
 pH 7.4, 30°C Homo sapiens methyl 2-(4-(3,3,3-trifluoro-2,2-dimethylpropanoyloxy)benzamido)benzoate
0.01
-
 pH 7.4, 30°C Homo sapiens ethyl 2-(4-(3,3,3-trifluoro-2,2-dimethylpropanoyloxy)benzamido)benzoate
0.01
-
 pH 7.4, 30°C Homo sapiens propyl 2-(4-(3,3,3-trifluoro-2,2-dimethylpropanoyloxy)benzamido)benzoate
0.01
-
 pH 7.4, 30°C Homo sapiens methyl 2-(4-pivalamidophenylsulfonamido)benzoate
0.01
-
 pH 7.4, 30°C Homo sapiens 4-(N-(2-acetylphenyl)sulfamoyl)phenyl 2-methylpropane-2-sulfinate
0.01
-
 pH 7.4, 30°C Homo sapiens 4-(N-(2-formylphenyl)sulfamoyl)phenyl 2-methylpropane-2-sulfinate

General Information

General Information Comment Organism
malfunction excessive release of proteases mediates tissue damage Homo sapiens