Cloned (Comment) | Organism |
---|---|
transient expression of the enzyme in COS7 cells | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(1H-benzo[d][1,2,3]triazol-1-yl)(4-(3-phenoxybenzyl)-piperazin-1-yl)-methanone | - |
Homo sapiens | |
(1H-benzo[d][1,2,3]triazol-1-yl)(4-(4-phenoxybenzyl)-piperazin-1-yl)-methanone hydrochloride | - |
Homo sapiens | |
(1H-imidazol-1-yl)(4-(3-phenoxybenzyl)piperazin-1-yl)methanone | - |
Homo sapiens | |
(1H-imidazol-1-yl)(4-(4-phenoxy-benzyl)-piperazin-1-yl)-methanone hydrochloride | - |
Homo sapiens | |
(3H-[1,2,3]triazol[4,5-b]pyridin-3-yl)(4-(3-phenoxybenzyl)-piperazin-1-yl)-methanone | - |
Homo sapiens | |
(4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)-piperidin-1-yl)(1H-1,2,4-triazol-1-yl)methanone | - |
Homo sapiens | |
(4-benzhydrylpiperazin-1-yl)(4-phenyl-1H-imidazol-1-yl)methanone | 62% activity remaining at 0.01 mM | Homo sapiens | |
(4-phenylpiperazin-1-yl)(1H-1,2,4-triazol-1-yl)methanone | - |
Homo sapiens | |
1,1,1,3,3,3-hexafluoropropan-2-yl 4-(3-phenoxybenzyl)piperazine-1-carboxylate | - |
Homo sapiens | |
1-[4-[bis(1,3-benzodioxol-5-yl)(hydroxy)methyl]piperidin-1-yl]-3,3,3-trifluoro-2-(trifluoromethyl)propan-1-one | - |
Homo sapiens | |
1H-benzotriazol-1-yl[4-(diphenylmethyl)piperazin-1-yl]methanone | - |
Homo sapiens | |
2,2,2-trichloroethyl 4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)piperidine-1-carboxylate | - |
Homo sapiens | |
2H-benzotriazol-2-yl(4-phenylpiperazin-1-yl)methanone | - |
Homo sapiens | |
2H-benzotriazol-2-yl[4-(diphenylmethyl)piperazin-1-yl]methanone | - |
Homo sapiens | |
4-(3-phenoxybenzyl)-N-(4-methoxyphenyl)piperazine-1-carboxamide | - |
Homo sapiens | |
4-(3-phenoxybenzyl)-N-(4-nitrophenyl)piperazine-1-carboxamide | - |
Homo sapiens | |
4-(3-phenoxybenzyl)-N-phenylpiperazine-1-carboxamide | - |
Homo sapiens | |
4-benzhydryl-N-(4-(trifluoromethyl)phenyl)piperazine-1-carboxamide | 86% activity remaining at 0.01 mM | Homo sapiens | |
4-benzhydryl-N-(4-butylphenyl)piperazine-1-carboxamide | 84% activity remaining at 0.01 mM | Homo sapiens | |
4-benzhydryl-N-(4-methoxyphenyl)piperazine-1-carboxamide | 89% activity remaining at 0.01 mM | Homo sapiens | |
4-benzhydryl-N-(4-nitrophenyl)piperazine-1-carboxamide | 84% activity remaining at 0.01 mM | Homo sapiens | |
4-benzhydryl-N-(pyridin-2-yl)piperazine-1-carboxamide | 87% activity remaining at 0.01 mM | Homo sapiens | |
4-benzhydryl-N-(pyridin-3-yl)piperazine-1-carboxamide | 87% activity remaining at 0.01 mM | Homo sapiens | |
4-benzhydryl-N-phenylpiperazine-1-carboxamide | 88% activity remaining at 0.01 mM | Homo sapiens | |
4-nitrophenyl 4-(3-phenoxybenzyl)piperazine-1-carboxylate | - |
Homo sapiens | |
4-nitrophenyl 4-(diphenylmethyl)piperazine-1-carboxylate | - |
Homo sapiens | |
4-nitrophenyl 4-[bis(1,3-benzodioxol-5-yl)(hydroxy)methyl]piperidine-1-carboxylate | - |
Homo sapiens | |
4-nitrophenyl 4-[bis(4-fluorophenyl)methyl]piperazine-1-carboxylate | - |
Homo sapiens | |
4-nitrophenyl-4-(4-phenoxy-benzyl)-piperazine-1-carboxylate | - |
Homo sapiens | |
4-nitrophenyl-4-(bis(benzo[d][1,3]dioxol-5-yl)methyl)piperidine-1-carboxylate | - |
Homo sapiens | |
4-[4-(2,4-difluorophenyl)-1,3-thiazol-2-yl]-N-(3,4-dimethyl-1,2-oxazol-5-yl)piperazine-1-carboxamide | - |
Homo sapiens | |
benzyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)-piperidine-1-carboxylate | - |
Homo sapiens | |
ethyl 4-(1H-1,2,4-triazol-1-ylcarbonyl)piperazine-1-carboxylate | - |
Homo sapiens | |
ethyl 4-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-ylcarbonyl)piperazine-1-carboxylate | - |
Homo sapiens | |
additional information | piperazine and piperidine carboxamides and carbamates as enzyme inhibitors, molecular modeling, overview. Diverse leaving groups are tolerated for FAAH inhibitors | Homo sapiens | |
N-(pyridin-3-yl)-4-(3-[[5-(trifluoromethyl)pyridin-2-yl]oxy]benzyl)piperidine-1-carboxamide | - |
Homo sapiens | |
N-phenyl-4-(3-phenyl-4,5-dihydro-1,2,4-thiadiazol-5-yl)piperazine-1-carboxamide | - |
Homo sapiens | |
[4-(3-phenoxybenzyl)piperazin-1-yl](1H-1,2,4-triazol-1-yl)methanone | - |
Homo sapiens | |
[4-(diphenylmethyl)piperazin-1-yl](1H-1,2,4-triazol-1-yl)methanone | - |
Homo sapiens | |
[4-(diphenylmethyl)piperazin-1-yl](1H-imidazol-1-yl)methanone | - |
Homo sapiens | |
[4-[bis(1,3-benzodioxol-5-yl)methyl]piperidin-1-yl](1H-1,2,4-triazol-1-yl)methanone | - |
Homo sapiens | |
[4-[bis(4-fluorophenyl)methyl]piperazin-1-yl](1H-1,2,4-triazol-1-yl)methanone | - |
Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | Homo sapiens | FAAH is the primary N-arachidonoylethanolamine-degrading enzyme, but it is also capable of hydrolyzing other bioactive N-acylethanolamines, such as N-palmitoylethanolamine, N-oleoylethanolamine and the sleep-inducing lipid oleamide | ? | - |
? | |
N-arachidonoylethanolamine + H2O | Homo sapiens | - |
arachidonic acid + ethanolamine | - |
? | |
N-oleoylethanolamine + H2O | Homo sapiens | - |
oleic acid + ethanolamine | - |
? | |
N-palmitoylethanolamine + H2O | Homo sapiens | - |
palmitic acid + ethanolamine | - |
? | |
oleamide + H2O | Homo sapiens | - |
oleic acid + NH3 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | O00519 | - |
- |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
additional information | FAAH is the primary N-arachidonoylethanolamine-degrading enzyme, but it is also capable of hydrolyzing other bioactive N-acylethanolamines, such as N-palmitoylethanolamine, N-oleoylethanolamine and the sleep-inducing lipid oleamide | Homo sapiens | ? | - |
? | |
N-arachidonoylethanolamine + H2O | - |
Homo sapiens | arachidonic acid + ethanolamine | - |
? | |
N-oleoylethanolamine + H2O | - |
Homo sapiens | oleic acid + ethanolamine | - |
? | |
N-palmitoylethanolamine + H2O | - |
Homo sapiens | palmitic acid + ethanolamine | - |
? | |
oleamide + H2O | - |
Homo sapiens | oleic acid + NH3 | - |
? |
Synonyms | Comment | Organism |
---|---|---|
FAAH | - |
Homo sapiens |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.00000163 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-nitrophenyl-4-(4-phenoxy-benzyl)-piperazine-1-carboxylate | |
0.00000175 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-(3-phenoxybenzyl)-N-(4-methoxyphenyl)piperazine-1-carboxamide | |
0.00000188 | - |
pH and temperature not specified in the publication | Homo sapiens | 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(3-phenoxybenzyl)piperazine-1-carboxylate | |
0.00000199 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-(3-phenoxybenzyl)-N-(4-nitrophenyl)piperazine-1-carboxamide | |
0.0000034 | - |
pH and temperature not specified in the publication | Homo sapiens | (1H-imidazol-1-yl)(4-(4-phenoxy-benzyl)-piperazin-1-yl)-methanone hydrochloride | |
0.000015 | - |
pH and temperature not specified in the publication | Homo sapiens | (1H-imidazol-1-yl)(4-(3-phenoxybenzyl)piperazin-1-yl)methanone | |
0.000023 | - |
pH and temperature not specified in the publication | Homo sapiens | (3H-[1,2,3]triazol[4,5-b]pyridin-3-yl)(4-(3-phenoxybenzyl)-piperazin-1-yl)-methanone | |
0.000089 | - |
pH and temperature not specified in the publication | Homo sapiens | (1H-benzo[d][1,2,3]triazol-1-yl)(4-(3-phenoxybenzyl)-piperazin-1-yl)-methanone | |
0.000708 | - |
pH and temperature not specified in the publication | Homo sapiens | (1H-benzo[d][1,2,3]triazol-1-yl)(4-(4-phenoxybenzyl)-piperazin-1-yl)-methanone hydrochloride | |
0.00162 | - |
pH and temperature not specified in the publication | Homo sapiens | (4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)-piperidin-1-yl)(1H-1,2,4-triazol-1-yl)methanone | |
0.00194 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-nitrophenyl-4-(bis(benzo[d][1,3]dioxol-5-yl)methyl)piperidine-1-carboxylate | |
0.00195 | - |
pH and temperature not specified in the publication | Homo sapiens | benzyl 4-(dibenzo[d][1,3]dioxol-5-yl(hydroxy)methyl)-piperidine-1-carboxylate | |
0.00196 | - |
pH and temperature not specified in the publication | Homo sapiens | 2,2,2-trichloroethyl 4-(bis(benzo[d][1,3]dioxol-5-yl)(hydroxy)methyl)piperidine-1-carboxylate | |
0.00302 | - |
pH and temperature not specified in the publication | Homo sapiens | 4-(3-phenoxybenzyl)-N-phenylpiperazine-1-carboxamide |
General Information | Comment | Organism |
---|---|---|
metabolism | fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL) are key hydrolytic enzymes of the endocannabinoid system | Homo sapiens |