Inhibitors | Comment | Organism | Structure |
---|---|---|---|
1-(2-((1-methyl-1H-imidazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione | - |
Homo sapiens | |
1-(2-((5-phenyl-1,3,4-oxadiazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione | - |
Homo sapiens | |
1-(2-((benzo[d]oxazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione | - |
Homo sapiens | |
1-(2-((benzo[d]thiazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione | - |
Homo sapiens | |
1-(4-((5-phenyl-1,3,4-oxadiazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione | - |
Homo sapiens | |
1-(4-((benzo[d]oxazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione | - |
Homo sapiens | |
1-(4-((benzo[d]thiazol-2-ylthio)methyl)phenyl)-3,3-diethylazetidine-2,4-dione | - |
Homo sapiens | |
1-(4-chlorophenyl)-3,3-diethylazetidine-2,4-dione | - |
Homo sapiens | |
1-(4-chlorophenyl)-3,3-dimethylazetidine-2,4-dione | - |
Homo sapiens | |
1-(6-((benzo[d]thiazol-2-ylthio)methyl)pyridin-3-yl)-3,3-diethylazetidine-2,4-dione | - |
Homo sapiens | |
1-benzyl-3,3-dimethylazetidine-2,4-dione | - |
Homo sapiens | |
2-(4-(3,3-diethyl-2,4-dioxoazetidin-1-yl)benzylthio)benzo[d ]-oxazole-6-carboxylic acid | - |
Homo sapiens | |
3,3-diethyl-1-(4-((phenylthio)methyl)phenyl)azetidine-2,4-dione | - |
Homo sapiens | |
3,3-diethyl-1-(4-methoxyphenyl)azetidine-2,4-dione | - |
Homo sapiens | |
3,3-diethyl-1-(4-methylphenyl)azetidine-2,4-dione | - |
Homo sapiens | |
3,3-diethyl-1-(6-methylpyridin-3-yl)azetidine-2,4-dione | - |
Homo sapiens | |
3,3-diethyl-1-(naphthalen-1-yl)azetidine-2,4-dione | - |
Homo sapiens | |
3,3-diethyl-1-(pyridin-3-yl)azetidine-2,4-dione | - |
Homo sapiens | |
3,3-diethyl-1-o-tolylazetidine-2,4-dione | - |
Homo sapiens | |
3,3-diethyl-1-phenylazetidine-2,4-dione | - |
Homo sapiens | |
3,3-diethyl-1-[4-(naphthalen-2-yloxy)phenyl]azetidine-2,4-dione | - |
Homo sapiens | |
3,3-dimethyl-1-phenylazetidine-2,4-dione | - |
Homo sapiens | |
3-benzyl-3-ethyl-1-phenylazetidine-2,4-dione | - |
Homo sapiens | |
3-benzyl-3-methyl-1-phenylazetidine-2,4-dione | - |
Homo sapiens | |
3-ethyl-3-isobutyl-1-phenylazetidine-2,4-dione | - |
Homo sapiens | |
4-(3,3-diethyl-2,4-dioxoazetidin-1-yl)benzonitrile | - |
Homo sapiens | |
ethyl [4-(3,3-diethyl-2,4-dioxoazetidin-1-yl)phenyl]acetate | - |
Homo sapiens | |
additional information | 4-oxo-beta-lactams are selective and potent inhibitors of leukocyte elastase, 4-oxo-beta-lactams containing a heteroarylthiomethyl group on the para position of an N1-aryl moiety afforded highly potent and selective inhibition of the enzyme, even at a very low inhibitor to enzyme ratio, structure-activity relationship analysis, inhibition mechanisms, molecular modelling, overview | Homo sapiens |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
extracellular | the enzyme is stored in and secreted from neutrophils | Homo sapiens | - |
- |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
neutrophil | - |
Homo sapiens | - |
plasma | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
N-methoxysuccinyl-Ala-Ala-Pro-Val-4-nitroanilide + H2O | - |
Homo sapiens | N-methoxysuccinyl-Ala-Ala-Pro-Val + 4-nitroaniline | - |
? |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Homo sapiens |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
additional information | - |
additional information | detailed inhibition kinetics of 4-oxo-beta-lactams, overview | Homo sapiens |
General Information | Comment | Organism |
---|---|---|
physiological function | leukocyte elastase is a serine protease stored in and secreted from neutrophils that plays a determinant role in the pathogenesis of several lung diseases | Homo sapiens |