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Literature summary for 3.5.1.99 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
Search for more literature for 3.5.1.99

Cloned(Commentary)

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

Inhibitors

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

Natural Substrates/ Products (Substrates)

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

Organism

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

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
FAAH
-
 Rattus norvegicus
FAAH
-
 Homo sapiens

Temperature Optimum [°C]

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

pH Optimum

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

IC50 Value

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