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Literature summary extracted from

  • Kono, M.; Matsumoto, T.; Imaeda, T.; Kawamura, T.; Fujimoto, S.; Kosugi, Y.; Odani, T.; Shimizu, Y.; Matsui, H.; Shimojo, M.; Kori, M.
    Design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors (2014), Bioorg. Med. Chem., 22, 1468-1478.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.5.1.99 cloning from a human brain library as cDNA library, recombinant stable expression in CHO-K1 cells Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.5.1.99 2-(methylamino)-2-oxoethyl [2-[1-(6-methylpyridin-2-yl)piperidin-4-yl]ethyl]carbamate
-
 Homo sapiens
3.5.1.99 2-(methylamino)-2-oxoethyl [2-[1-(6-methylpyridin-2-yl)piperidin-4-yl]ethyl]carbamate
-
 Rattus norvegicus
3.5.1.99 3'-carbamoylbiphenyl-3-yl cyclohexylcarbamate
-
 Rattus norvegicus
3.5.1.99 4-(3-phenyl-1,2,4-thiadiazol-5-yl)-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Homo sapiens
3.5.1.99 4-(3-phenyl-1,2,4-thiadiazol-5-yl)-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 4-[2-(2,4-difluorophenyl)pyridin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Homo sapiens
3.5.1.99 4-[2-(2,4-difluorophenyl)pyridin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 4-[2-(2,4-difluorophenyl)pyrimidin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Homo sapiens
3.5.1.99 4-[2-(2,4-difluorophenyl)pyrimidin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 4-[3-(4-chlorophenoxy)benzyl]-N-(pyridin-3-yl)piperazine-1-carboxamide
-
 Homo sapiens
3.5.1.99 4-[3-(4-chlorophenoxy)benzyl]-N-(pyridin-3-yl)piperazine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 4-[4-(2,3-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Homo sapiens
3.5.1.99 4-[4-(2,3-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 4-[4-(2,4-difluorophenyl)-1,3-thiazol-2-yl]-N-(3,4-dimethyl-1,2-oxazol-5-yl)piperazine-1-carboxamide
-
 Homo sapiens
3.5.1.99 4-[4-(2,4-difluorophenyl)-1,3-thiazol-2-yl]-N-(3,4-dimethyl-1,2-oxazol-5-yl)piperazine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 4-[4-(2,4-difluorophenyl)pyridin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Homo sapiens
3.5.1.99 4-[4-(2,4-difluorophenyl)pyridin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 4-[4-(2,4-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Homo sapiens
3.5.1.99 4-[4-(2,4-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 4-[4-(2,5-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Homo sapiens
3.5.1.99 4-[4-(2,5-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 4-[4-(3,4-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide analgesic effect of 21d in rat inflammatory pain model, overview Homo sapiens
3.5.1.99 4-[4-(3,4-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 4-[4-(3,5-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Homo sapiens
3.5.1.99 4-[4-(3,5-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 4-[6-(2,4-difluorophenyl)pyridin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Homo sapiens
3.5.1.99 4-[6-(2,4-difluorophenyl)pyridin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 4-[6-(2,4-difluorophenyl)pyrimidin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Homo sapiens
3.5.1.99 4-[6-(2,4-difluorophenyl)pyrimidin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 7-phenyl-1-[5-(pyridin-2-yl)-1,3-oxazol-2-yl]heptan-1-one
-
 Homo sapiens
3.5.1.99 7-phenyl-1-[5-(pyridin-2-yl)-1,3-oxazol-2-yl]heptan-1-one
-
 Rattus norvegicus
3.5.1.99 additional information design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors, overview Homo sapiens
3.5.1.99 additional information design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors, overview Rattus norvegicus
3.5.1.99 N-(3,4-dimethyl-1,2-oxazol-5-yl)-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
-
 Homo sapiens
3.5.1.99 N-(3,4-dimethyl-1,2-oxazol-5-yl)-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 N-(pyridazin-3-yl)-4-(3-[[5-(trifluoromethyl)pyridin-2-yl]oxy]benzylidene)piperidine-1-carboxamide
-
 Homo sapiens
3.5.1.99 N-(pyridazin-3-yl)-4-(3-[[5-(trifluoromethyl)pyridin-2-yl]oxy]benzylidene)piperidine-1-carboxamide
-
 Rattus norvegicus
3.5.1.99 N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
-
 Homo sapiens
3.5.1.99 N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
-
 Rattus norvegicus

Natural Substrates/ Products (Substrates)

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

Organism

EC Number Organism UniProt Comment Textmining
3.5.1.99 Homo sapiens O00519
-
-
3.5.1.99 Rattus norvegicus P97612
-
-
3.5.1.99 Rattus norvegicus Sprague-Dawley P97612
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.5.1.99 anandamide + H2O
-
 Rattus norvegicus ethanolamine + arachidonic acid
-
 ?
3.5.1.99 anandamide + H2O
-
 Homo sapiens ethanolamine + arachidonic acid
-
 ?
3.5.1.99 anandamide + H2O
-
 Rattus norvegicus Sprague-Dawley ethanolamine + arachidonic acid
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.5.1.99 FAAH
-
 Rattus norvegicus
3.5.1.99 FAAH
-
 Homo sapiens

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.5.1.99 37
-
 assay at Rattus norvegicus
3.5.1.99 37
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.5.1.99 9
-
 assay at Rattus norvegicus
3.5.1.99 9
-
 assay at Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.5.1.99 0.000000025
-
 pH 9.0, 37°C Homo sapiens 4-[4-(2,5-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.000000072
-
 pH 9.0, 37°C Homo sapiens 4-[4-(2,3-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.00000017
-
 pH 9.0, 37°C Rattus norvegicus 4-[4-(2,5-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.00000028
-
 pH 9.0, 37°C Rattus norvegicus 4-[4-(3,4-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.00000034
-
 pH 9.0, 37°C Rattus norvegicus 4-[4-(3,5-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.00000043
-
 pH 9.0, 37°C Homo sapiens 4-[4-(2,4-difluorophenyl)-1,3-thiazol-2-yl]-N-(3,4-dimethyl-1,2-oxazol-5-yl)piperazine-1-carboxamide
3.5.1.99 0.00000043
-
 pH 9.0, 37°C Rattus norvegicus 4-[4-(2,4-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.00000046
-
 pH 9.0, 37°C Rattus norvegicus 4-[4-(2,4-difluorophenyl)-1,3-thiazol-2-yl]-N-(3,4-dimethyl-1,2-oxazol-5-yl)piperazine-1-carboxamide
3.5.1.99 0.00000072
-
 pH 9.0, 37°C Homo sapiens 4-[4-(3,4-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.0000008
-
 pH 9.0, 37°C Homo sapiens 4-[4-(3,5-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.0000011
-
 pH 9.0, 37°C Homo sapiens 4-[4-(2,4-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.0000012
-
 pH 9.0, 37°C Rattus norvegicus 4-[4-(2,3-difluorophenyl)pyrimidin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.0000012
-
 pH 9.0, 37°C Rattus norvegicus N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
3.5.1.99 0.0000013
-
 pH 9.0, 37°C Rattus norvegicus N-(3,4-dimethyl-1,2-oxazol-5-yl)-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
3.5.1.99 0.0000015
-
 pH 9.0, 37°C Homo sapiens 4-[6-(2,4-difluorophenyl)pyrimidin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.0000017
-
 pH 9.0, 37°C Rattus norvegicus 4-[6-(2,4-difluorophenyl)pyrimidin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.0000017
-
 pH 9.0, 37°C Homo sapiens N-(3,4-dimethyl-1,2-oxazol-5-yl)-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
3.5.1.99 0.0000022
-
 pH 9.0, 37°C Homo sapiens 4-[4-(2,4-difluorophenyl)pyridin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.0000029
-
 pH 9.0, 37°C Homo sapiens 4-(3-phenyl-1,2,4-thiadiazol-5-yl)-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.0000033
-
 pH 9.0, 37°C Rattus norvegicus 4-(3-phenyl-1,2,4-thiadiazol-5-yl)-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.0000043
-
 pH 9.0, 37°C Rattus norvegicus 4-[4-(2,4-difluorophenyl)pyridin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.000011
-
 pH 9.0, 37°C Homo sapiens N-phenyl-4-(3-phenyl-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide
3.5.1.99 0.000012
-
 pH 9.0, 37°C Rattus norvegicus 4-[2-(2,4-difluorophenyl)pyridin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.000013
-
 pH 9.0, 37°C Rattus norvegicus 4-[6-(2,4-difluorophenyl)pyridin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.000023
-
 pH 9.0, 37°C Homo sapiens 4-[2-(2,4-difluorophenyl)pyrimidin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.000028
-
 pH 9.0, 37°C Homo sapiens 4-[2-(2,4-difluorophenyl)pyridin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.000034
-
 pH 9.0, 37°C Rattus norvegicus 4-[2-(2,4-difluorophenyl)pyrimidin-4-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.000036
-
 pH 9.0, 37°C Homo sapiens 4-[6-(2,4-difluorophenyl)pyridin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.000074
-
 pH 9.0, 37°C Rattus norvegicus 4-[4-(2,4-difluorophenyl)pyridin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide
3.5.1.99 0.00014
-
 pH 9.0, 37°C Homo sapiens 4-[4-(2,4-difluorophenyl)pyridin-2-yl]-N-(pyridazin-3-yl)piperazine-1-carboxamide