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Literature summary for 3.5.1.99 extracted from

  • Watabiki, T.; Tsuji, N.; Kiso, T.; Ozawa, T.; Narazaki, F.; Kakimoto, S.
    In vitro and in vivo pharmacological characterization of ASP8477 A novel highly selective fatty acid amide hydrolase inhibitor (2017), Eur. J. Pharmacol., 815, 42-48 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
3-pyridyl 4-(phenylcarbamoyl)piperidine-1-carboxylate i.e. ASP8477; i.e. ASP8477 Homo sapiens
3-pyridyl 4-(phenylcarbamoyl)piperidine-1-carboxylate i.e. ASP8477 Rattus norvegicus
pyridin-3-yl 4-(phenylcarbamoyl)piperidine-1-carboxylate
-
Homo sapiens
pyridin-3-yl 4-(phenylcarbamoyl)piperidine-1-carboxylate
-
Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
anandamide + H2O Rattus norvegicus
-
arachidonic acid + ethanolamine
-
?
anandamide + H2O Homo sapiens
-
arachidonic acid + ethanolamine
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens B2C6G4
-
-
Homo sapiens O00519
-
-
Rattus norvegicus P97612
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
anandamide + H2O
-
Rattus norvegicus arachidonic acid + ethanolamine
-
?
anandamide + H2O
-
Homo sapiens arachidonic acid + ethanolamine
-
?
oleoylethanolamide + H2O
-
Rattus norvegicus oleic acid + ethanolamine
-
?
oleoylethanolamide + H2O
-
Homo sapiens oleic acid + ethanolamine
-
?

Synonyms

Synonyms Comment Organism
FAAH
-
Rattus norvegicus
FAAH-1
-
Homo sapiens
FAAH-2
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000165
-
pyridin-3-yl 4-(phenylcarbamoyl)piperidine-1-carboxylate 37°C, pH 8.0, mutant enzyme P129T Homo sapiens
0.00000399
-
pyridin-3-yl 4-(phenylcarbamoyl)piperidine-1-carboxylate 37°C, pH 8.0, wild-type enzyme Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00000165
-
pH 8.0, 37°C, mutant enzyme P129T Homo sapiens 3-pyridyl 4-(phenylcarbamoyl)piperidine-1-carboxylate
0.00000399
-
pH 8.0, 37°C, wild-type enzyme Homo sapiens 3-pyridyl 4-(phenylcarbamoyl)piperidine-1-carboxylate
0.00000442
-
37°C, pH 8.0 Rattus norvegicus pyridin-3-yl 4-(phenylcarbamoyl)piperidine-1-carboxylate
0.00000442
-
pH 8.0, 37°C, wild-type enzyme Rattus norvegicus 3-pyridyl 4-(phenylcarbamoyl)piperidine-1-carboxylate
0.0000573
-
37°C, pH 8.0 Homo sapiens pyridin-3-yl 4-(phenylcarbamoyl)piperidine-1-carboxylate
0.0000573
-
pH 8.0, 37°C, wild-type enzyme Homo sapiens 3-pyridyl 4-(phenylcarbamoyl)piperidine-1-carboxylate

General Information

General Information Comment Organism
physiological function primary catabolic enzyme for anandamide, an endogenous cannabinoid Rattus norvegicus
physiological function primary catabolic enzyme for anandamide, an endogenous cannabinoid Homo sapiens