EC Number | Cloned (Comment) | Organism |
---|---|---|
3.5.1.99 | recombinant expression of FAAH-1 in HEK-293 cells | Homo sapiens |
EC Number | Inhibitors | Comment | Organism | Structure |
---|---|---|---|---|
3.5.1.99 | (1-benzhydryltriazol-4-yl)methyl N-cyclohexylcarbamate | 73% inhibition at 0.1 mM | Homo sapiens | |
3.5.1.99 | (1-benzyltriazol-4-yl)methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | (1-phenethyltriazol-4-yl)methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | (1-phenyltriazol-4-yl)methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | (3-phenylphenyl)methyl N-cyclohexylcarbamate | 65% inhibition at 0.1 mM | Homo sapiens | |
3.5.1.99 | (benzyl-1,2,4-triazol-3-yl)methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | 1-(1-phenyl-1,2,4-triazol-3-yl)methyl N-cyclohexylcarbamate | 70% inhibition at 0.1 mM | Homo sapiens | |
3.5.1.99 | 2-(1-benzyltriazol-4-yl)ethyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | 2-(1-phenyltriazol-4-yl)ethyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | 3'-carbamoylbiphenyl-3-yl cyclohexylcarbamate | exerts a combination of anxiolytic-like, anti-depressant-like, and analgesic effects, due to its ability to inhibit FAAH activity in the CNS and peripheral tissues. Covalent enzyme binding at Ser241 leading to irreversible inhibition, the attack at the carbonyl group by Ser 241 leads to the formation of carbamoylated, catalytically inactive FAAH and releasing the O-biphenyl moiety as the leaving group | Homo sapiens | |
3.5.1.99 | 3'-carbamoylbiphenyl-3-yl cyclohexylcarbamate | covalent enzyme binding at Ser241 leading to irreversible inhibition, the attack at the carbonyl group by Ser 241 leads to the formation of carbamoylated, catalytically inactive FAAH and releasing the O-biphenyl moiety as the leaving group | Rattus norvegicus | |
3.5.1.99 | 6-hydroxybiphenyl-3-yl cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | 6-hydroxybiphenyl-3-yl cyclohexylcarbamate | - |
Rattus norvegicus | |
3.5.1.99 | biphenyl-3-yl cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | biphenyl-3-yl cyclohexylcarbamate | - |
Rattus norvegicus | |
3.5.1.99 | additional information | O-(triazolyl)methyl carbamates as potent fatty acid amide hydrolase inhibitors, overview | Homo sapiens | |
3.5.1.99 | additional information | O-(triazolyl)methyl carbamates as potent fatty acid amide hydrolase inhibitors, overview. These compounds show improved stability in rat plasma and kinetic solubility in buffer with respect to the lead compound O-(1,2,3-triazol-4-yl)methyl carbamate | Rattus norvegicus | |
3.5.1.99 | [1-(2-naphthylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-(m-tolylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-(o-tolylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-(p-tolylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(2,6-difluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(2,6-difluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Rattus norvegicus | |
3.5.1.99 | [1-[(2-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(2-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Rattus norvegicus | |
3.5.1.99 | [1-[(2-cyanophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(2-fluoro-3-methoxy-phenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(2-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(2-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Rattus norvegicus | |
3.5.1.99 | [1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Rattus norvegicus | |
3.5.1.99 | [1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | - |
Rattus norvegicus | |
3.5.1.99 | [1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | - |
Rattus norvegicus | |
3.5.1.99 | [1-[(3,5-difluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(3,5-difluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Rattus norvegicus | |
3.5.1.99 | [1-[(3,5-dimethoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(3,5-dimethoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Rattus norvegicus | |
3.5.1.99 | [1-[(3-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(3-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Rattus norvegicus | |
3.5.1.99 | [1-[(3-cyanophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(3-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(3-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Rattus norvegicus | |
3.5.1.99 | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Rattus norvegicus | |
3.5.1.99 | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | - |
Rattus norvegicus | |
3.5.1.99 | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | - |
Rattus norvegicus | |
3.5.1.99 | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | - |
Rattus norvegicus | |
3.5.1.99 | [1-[(4-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(4-cyanophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(4-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens | |
3.5.1.99 | [1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | - |
Homo sapiens |
EC Number | Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|---|
3.5.1.99 | membrane | bound | Rattus norvegicus | 16020 | - |
3.5.1.99 | membrane | bound | Homo sapiens | 16020 | - |
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 SpragueDawley | - |
ethanolamine + arachidonic acid | - |
? | |
3.5.1.99 | N-arachidonoylethanolamine + H2O | Rattus norvegicus | - |
arachidonic acid + ethanolamine | - |
? | |
3.5.1.99 | N-arachidonoylethanolamine + H2O | Rattus norvegicus SpragueDawley | - |
arachidonic acid + ethanolamine | - |
? |
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 SpragueDawley | P97612 | - |
- |
EC Number | Purification (Comment) | Organism |
---|---|---|
3.5.1.99 | recombinant FAAH-1 partially from HEK-293 cells by membrane preparation | Homo sapiens |
EC Number | Source Tissue | Comment | Organism | Textmining |
---|---|---|---|---|
3.5.1.99 | brain | - |
Rattus norvegicus | - |
3.5.1.99 | brain | - |
Homo sapiens | - |
3.5.1.99 | liver | - |
Homo sapiens | - |
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 SpragueDawley | ethanolamine + arachidonic acid | - |
? | |
3.5.1.99 | N-arachidonoylethanolamine + H2O | - |
Rattus norvegicus | arachidonic acid + ethanolamine | - |
? | |
3.5.1.99 | N-arachidonoylethanolamine + H2O | - |
Rattus norvegicus SpragueDawley | arachidonic acid + ethanolamine | - |
? |
EC Number | Synonyms | Comment | Organism |
---|---|---|---|
3.5.1.99 | FAAH | - |
Rattus norvegicus |
3.5.1.99 | FAAH | - |
Homo sapiens |
3.5.1.99 | FAAH-1 | - |
Homo sapiens |
EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|---|
3.5.1.99 | 37 | - |
assay at | Rattus norvegicus |
EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|---|
3.5.1.99 | 7.4 | - |
assay at | Rattus norvegicus |
EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|---|
3.5.1.99 | 0.0000014 | - |
pH 7.4, 37°C | Rattus norvegicus | [1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000014 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000032 | - |
pH 7.4, 37°C | Rattus norvegicus | [1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | |
3.5.1.99 | 0.0000032 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | |
3.5.1.99 | 0.0000036 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(3,5-dimethoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000039 | - |
pH 7.4, 37°C | Rattus norvegicus | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | |
3.5.1.99 | 0.0000039 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | |
3.5.1.99 | 0.0000057 | - |
pH 7.4, 37°C | Rattus norvegicus | biphenyl-3-yl cyclohexylcarbamate | |
3.5.1.99 | 0.0000058 | - |
pH 7.4, 37°C | Rattus norvegicus | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | |
3.5.1.99 | 0.0000058 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | |
3.5.1.99 | 0.0000062 | - |
pH 7.4, 37°C | Rattus norvegicus | [1-[(2-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000062 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(2-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000076 | - |
pH 7.4, 37°C | Rattus norvegicus | [1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | |
3.5.1.99 | 0.0000076 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | |
3.5.1.99 | 0.0000098 | - |
pH 7.4, 37°C | Rattus norvegicus | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | |
3.5.1.99 | 0.0000098 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | |
3.5.1.99 | 0.0000099 | - |
pH 7.4, 37°C | Rattus norvegicus | [1-[(2-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000099 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(2-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000104 | - |
pH 7.4, 37°C | Rattus norvegicus | [1-[(3,5-difluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000104 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(3,5-difluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000105 | - |
pH 7.4, 37°C | Rattus norvegicus | [1-[(3,5-dimethoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000118 | - |
pH 7.4, 37°C | Rattus norvegicus | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000118 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(3-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000119 | - |
pH 7.4, 37°C | Rattus norvegicus | [1-[(2,6-difluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000119 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(2,6-difluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000121 | - |
pH 7.4, 37°C | Rattus norvegicus | [1-[(3-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000121 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(3-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000132 | - |
pH 7.4, 37°C | Rattus norvegicus | [1-[(3-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000132 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(3-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000195 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(2-cyanophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000215 | - |
pH 7.4, 37°C | Homo sapiens | [1-(o-tolylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000215 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(3-cyanophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000245 | - |
pH 7.4, 37°C | Homo sapiens | [1-(m-tolylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000446 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(2-fluoro-3-methoxy-phenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0000955 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(4-fluorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.000154 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl N-[[1-[(2-methoxyphenyl)methyl]triazol-4-yl]methyl]carbamate | |
3.5.1.99 | 0.000215 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(4-chlorophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.0005 | - |
pH 7.4, 37°C | Homo sapiens | [1-(p-tolylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.000627 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(4-methoxyphenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.002 | - |
pH 7.4, 37°C | Homo sapiens | [1-(2-naphthylmethyl)triazol-4-yl]methyl N-cyclohexylcarbamate | |
3.5.1.99 | 0.002282 | - |
pH 7.4, 37°C | Homo sapiens | [1-[(4-cyanophenyl)methyl]triazol-4-yl]methyl N-cyclohexylcarbamate |
EC Number | General Information | Comment | Organism |
---|---|---|---|
3.5.1.99 | additional information | the active site of FAAH is characterized by an atypical catalytic triad, consisting of Ser241-Ser217-Ly142, which is capable of hydrolyzing amide and ester bonds at similar rates | Rattus norvegicus |
3.5.1.99 | additional information | the active site of FAAH is characterized by an atypical catalytic triad, consisting of Ser241-Ser217-Ly142, which is capable of hydrolyzing amide and ester bonds at similar rates | Homo sapiens |