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Literature summary for 3.5.1.99 extracted from

  • Dato, F.M.; Maassen, A.; Goldfuss, B.; Pietsch, M.
    Characterization of fatty acid amide hydrolase activity by a fluorescence-based assay (2018), Anal. Biochem., 546, 50-57 .
    View publication on PubMed
Search for more literature for 3.5.1.99

Application

Application Comment Organism
medicine fatty acid amide hydrolase is involved in many human diseases, particularly cancer, pain and inflammation as well as neurological, metabolic and cardiovascular disorders. Therefore, FAAH is an attractive target for the development of low-molecular-weight inhibitors as therapeutics, which requires robust assays that can be used for high-throughput screening of compound libraries. A highly sensitive fluorescence-based assay with the substrate N-(6-methoxypyridin-3-yl)decanamide is described Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-[(3R)-1-[4-(1-benzofuran-2-yl)pyrimidin-2-yl]piperidin-3-yl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one
-
 Homo sapiens
3'-carbamoyl[1,1'-biphenyl]-3-yl cyclohexylcarbamate
-
 Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.00843
-
 N-(6-methoxypyridin-3-yl)decanamide pH 8.0, 30°C Homo sapiens
0.16
-
 N-(6-methoxypyridin-3-yl)octanamide pH 8.0, 30°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Specific Activity [micromol/min/mg]

Specific Activity Minimum [µmol/min/mg] Specific Activity Maximum [µmol/min/mg] Comment Organism
0.00908
-
 Vmax, substrate: N-(6-methoxypyridin-3-yl)decanamide, pH 8.0, 30°C Homo sapiens
0.0213
-
 Vmax, substrate: N-(6-methoxypyridin-3-yl)octanamide, pH 8.0, 30°C Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-(4-nitrophenyl)decanamide + H2O
-
 Homo sapiens ?
-
 ?
N-(4-nitrophenyl)octanamide + H2O
-
 Homo sapiens ?
-
 ?
N-(6-methoxypyridin-3-yl)decanamide + H2O
-
 Homo sapiens ?
-
 ?
N-(6-methoxypyridin-3-yl)octanamide + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
FAAH
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000884
-
 pH 8.0, 30°C, substrate: N-(6-methoxypyridin-3-yl)octanamide Homo sapiens 3'-carbamoyl[1,1'-biphenyl]-3-yl cyclohexylcarbamate
0.000112
-
 pH 8.0, 30°C, substrate: N-(6-methoxypyridin-3-yl)decanamide Homo sapiens 3'-carbamoyl[1,1'-biphenyl]-3-yl cyclohexylcarbamate
0.00211
-
 pH 8.0, 30°C, substrate: N-(6-methoxypyridin-3-yl)octanamide Homo sapiens 1-[(3R)-1-[4-(1-benzofuran-2-yl)pyrimidin-2-yl]piperidin-3-yl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one
0.99146
-
 pH 8.0, 30°C, substrate: N-(6-methoxypyridin-3-yl)decanamide Homo sapiens 1-[(3R)-1-[4-(1-benzofuran-2-yl)pyrimidin-2-yl]piperidin-3-yl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one

General Information

General Information Comment Organism
metabolism the enzyme is involved in many human diseases, particularly cancer, pain and inflammation as well as neurological, metabolic and cardiovascular disorders Homo sapiens