Cloned (Comment) | Organism |
---|---|
recombinant expression in HEK-293 cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(7E)-N-[(3S)-2-oxoazetidin-3-yl]non-7-enamide | - |
Homo sapiens | |
(Z)-N-[(S)-2-oxoazetidin-3-yl]non-3-enamide | - |
Homo sapiens | |
1-heptyl-3-[(S)-2-oxoazetidin-3-yl]urea | - |
Homo sapiens | |
2,2-dimethyl-N-[(3S)-2-oxoazetidin-3-yl]nonanamide | - |
Homo sapiens | |
2-methyl-N-[(3S)-2-oxoazetidin-3-yl]nonanamide | - |
Homo sapiens | |
3-amino-N-nonanoyl-L-alanine | - |
Homo sapiens | |
4-butyl-N-[(S)-2-oxoazetidin-3-yl]benzamide | - |
Homo sapiens | |
5-phenylpentyl N-[(2S,3R)-2-methyl-4-oxo-oxetan-3-yl]-carbamate | - |
Homo sapiens | |
7-cyclohexyl-N-[(3S)-2-oxoazetidin-3-yl]heptanamide | - |
Homo sapiens | |
heptyl N-[(S)-2-oxoazetidin-3-yl]carbamate | - |
Homo sapiens | |
additional information | synthesis and evaluation of a series of N-(2-oxoazetidin-3-yl)amides as a novel class of enzyme inhibitors with good potency and improved physicochemical properties, suitable for systemic administration. No inhibition by 3-phenyl-N-[(S)-2-oxoazetidin-3-yl]propanamide, N-[(3S)-2-oxoazetidin-3-yl][1,1'-biphenyl]-4-carboxamide, N-(2-oxocyclobutyl)nonanamide, N-(azetidin-3-yl)nonanamide, 3-amino-N-nonanoyl-L-alanine, N-[(3S)-2-oxopyrrolidin-3-yl]nonanamide, N-[(S)-1-methyl-2-oxo-azetidin-3-yl]nonanamide, N-methyl-N-[(S)-2-oxoazetidin-3-yl]nonanamide, and (S)-3-(nonylamino)azetidin-2-one | Homo sapiens | |
N-(2-oxocyclobutyl)nonanamide | - |
Homo sapiens | |
N-(azetidin-3-yl)nonanamide | - |
Homo sapiens | |
N-[(3R)-2-oxoazetidin-3-yl]nonanamide | - |
Homo sapiens | |
N-[(3S)-2-oxoazetidin-3-yl]-4-phenylbutanamide | - |
Homo sapiens | |
N-[(3S)-2-oxoazetidin-3-yl]-5-phenylpentanamide | - |
Homo sapiens | |
N-[(3S)-2-oxoazetidin-3-yl]-6-phenylhexanamide | - |
Homo sapiens | |
N-[(3S)-2-oxoazetidin-3-yl]decanamide | - |
Homo sapiens | |
N-[(3S)-2-oxoazetidin-3-yl]heptanamide | - |
Homo sapiens | |
N-[(3S)-2-oxoazetidin-3-yl]nonanamide | - |
Homo sapiens | |
N-[(3S)-2-oxoazetidin-3-yl]octanamide | - |
Homo sapiens | |
N-[(3S)-2-oxoazetidin-3-yl]undecanamide | - |
Homo sapiens | |
N-[(S)-2-oxoazetidin-3-yl]-6-phenylhexanamide | - |
Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | Q02083 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
spleen | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
N-(4-methylcoumarin)palmitamide + H2O | - |
Homo sapiens | palmitic acid + 7-amino-4-methylcoumarin | - |
? |
Synonyms | Comment | Organism |
---|---|---|
N-acylethanolamine acid amidase | - |
Homo sapiens |
NAAA | - |
Homo sapiens |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Homo sapiens |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
4.5 | - |
assay at | Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0001 | - |
pH 5.0, 37°C | Homo sapiens | N-[(3S)-2-oxoazetidin-3-yl]undecanamide | |
0.00022 | - |
pH 5.0, 37°C | Homo sapiens | 2-methyl-N-[(3S)-2-oxoazetidin-3-yl]nonanamide | |
0.00024 | - |
pH 5.0, 37°C | Homo sapiens | heptyl N-[(S)-2-oxoazetidin-3-yl]carbamate | |
0.00024 | - |
pH 5.0, 37°C | Homo sapiens | N-[(3S)-2-oxoazetidin-3-yl]decanamide | |
0.00028 | - |
pH 5.0, 37°C | Homo sapiens | 7-cyclohexyl-N-[(3S)-2-oxoazetidin-3-yl]heptanamide | |
0.00034 | - |
pH 5.0, 37°C | Homo sapiens | N-[(3S)-2-oxoazetidin-3-yl]nonanamide | |
0.0006 | - |
pH 5.0, 37°C | Homo sapiens | N-[(3S)-2-oxoazetidin-3-yl]-6-phenylhexanamide | |
0.00076 | - |
pH 5.0, 37°C | Homo sapiens | 2,2-dimethyl-N-[(3S)-2-oxoazetidin-3-yl]nonanamide | |
0.0019 | - |
pH 5.0, 37°C | Homo sapiens | N-[(3S)-2-oxoazetidin-3-yl]octanamide | |
0.00309 | - |
pH 5.0, 37°C | Homo sapiens | (7E)-N-[(3S)-2-oxoazetidin-3-yl]non-7-enamide | |
0.0039 | - |
pH 5.0, 37°C | Homo sapiens | (Z)-N-[(S)-2-oxoazetidin-3-yl]non-3-enamide | |
0.00576 | - |
pH 5.0, 37°C | Homo sapiens | 1-heptyl-3-[(S)-2-oxoazetidin-3-yl]urea | |
0.0121 | - |
pH 5.0, 37°C | Homo sapiens | N-[(S)-2-oxoazetidin-3-yl]-6-phenylhexanamide | |
0.0138 | - |
pH 5.0, 37°C | Homo sapiens | 4-butyl-N-[(S)-2-oxoazetidin-3-yl]benzamide | |
0.027 | - |
pH 5.0, 37°C | Homo sapiens | N-[(3S)-2-oxoazetidin-3-yl]heptanamide | |
0.0272 | - |
pH 5.0, 37°C | Homo sapiens | N-[(3S)-2-oxoazetidin-3-yl]-5-phenylpentanamide | |
0.05 | - |
pH 4.5, 37°C | Homo sapiens | 5-phenylpentyl N-[(2S,3R)-2-methyl-4-oxo-oxetan-3-yl]-carbamate | |
0.0734 | - |
pH 5.0, 37°C | Homo sapiens | N-[(3S)-2-oxoazetidin-3-yl]-4-phenylbutanamide | |
0.0745 | - |
pH 5.0, 37°C | Homo sapiens | N-[(3R)-2-oxoazetidin-3-yl]nonanamide |
General Information | Comment | Organism |
---|---|---|
evolution | the enzyme is a cysteine amidase that belongs to the N-terminal nucleophile (Ntn) family of enzymes and is characterized by a conserved amino acid catalytic triad Cys, Arg, and Asp | Homo sapiens |