Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(R,S)-ibuprofen | - |
Rattus norvegicus | |
4-(acetylamino)phenyl (4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)acetate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl 2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanoate | competitive, also able to inhibit the FAAH activity in rat basophilic leukemia cells as assessed by measuring either the hydrolysis of anandamide, the FAAH-dependent cellular accumulation of anandamide, or the FAAH-dependent recycling of tritium to the cellmembranes | Rattus norvegicus | |
4-(acetylamino)phenyl 2-[[2-(trifluoromethyl)pyridin-4-yl]amino]pyridine-3-carboxylate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl 2-[[3-(trifluoromethyl)phenyl]amino]benzoate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl 2-[[3-(trifluoromethyl)phenyl]amino]pyridine-3-carboxylate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl 2-{[2-(trifluoromethyl)pyridin-4-yl]amino}benzoate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl 3-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanoate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl 3-methyl-4-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl 3-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl 4-([[2-(trifluoromethyl)pyridin-4-yl]amino]methyl)benzoate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl 4-chloro-2-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl 4-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl 5-chloro-2-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl 5-methyl-2-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl N-(3-methyl-4-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoyl)glycinate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl N-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoyl)glycinate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl N-[(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)acetyl]glycinate | - |
Rattus norvegicus | |
4-(acetylamino)phenyl N-[2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanoyl]glycinate | - |
Rattus norvegicus | |
additional information | paracetamol itself does not inhibit FAAH, but undergoes a FAAH-dependent two-step metabolic transformation in the brain, liver, and spinal cord to form the bioactive N-acylphenolamine AM404. Synthesis and evaluation of paracetamol ester enzyme inhibitors, structure-activity relationship studies, overview | Rattus norvegicus | |
N-(3-methylpyridin-2-yl)-2-(4'-isobutylphenyl)propionamide | i.e. Ibu-am5 | Rattus norvegicus | |
N-(4-hydroxyphenyl)-5Z,8Z,11Z,14Z-eicosatetraenamide | i.e. AM404, a bioactive N-acylphenolamine, derived from paracetamol, competitve inhibition | Rattus norvegicus |
Localization | Comment | Organism | GeneOntology No. | Textmining |
---|---|---|---|---|
membrane | - |
Rattus norvegicus | 16020 | - |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
anandamide + H2O | Rattus norvegicus | - |
arachidonic acid + ethanolamine | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Rattus norvegicus | - |
- |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
basophilic leukemia cell | - |
Rattus norvegicus | - |
brain | - |
Rattus norvegicus | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
anandamide + H2O | - |
Rattus norvegicus | arachidonic acid + ethanolamine | - |
? |
Synonyms | Comment | Organism |
---|---|---|
FAAH | - |
Rattus norvegicus |
Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
---|---|---|---|
37 | - |
assay at | Rattus norvegicus |
pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
---|---|---|---|
7.4 | - |
assay at | Rattus norvegicus |
Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
---|---|---|---|---|---|
0.00016 | - |
4-(acetylamino)phenyl 2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanoate | pH 7.4, 37°C | Rattus norvegicus |
IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
---|---|---|---|---|---|
0.0001 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl 2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanoate | |
0.00018 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl (4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)acetate | |
0.00073 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl N-[2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanoyl]glycinate | |
0.00087 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl N-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoyl)glycinate | |
0.0013 | - |
pH 7.4, 37°C | Rattus norvegicus | N-(3-methylpyridin-2-yl)-2-(4'-isobutylphenyl)propionamide | |
0.0015 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl 3-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanoate | |
0.0026 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl N-[(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)acetyl]glycinate | |
0.0027 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl 4-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoate | |
0.003 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl N-(3-methyl-4-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoyl)glycinate | |
0.0043 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl 5-chloro-2-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoate | |
0.0046 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl 3-methyl-4-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoate | |
0.0087 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl 2-[[3-(trifluoromethyl)phenyl]amino]benzoate | |
0.022 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl 4-([[2-(trifluoromethyl)pyridin-4-yl]amino]methyl)benzoate | |
0.031 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl 4-chloro-2-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoate | |
0.038 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl 5-methyl-2-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoate | |
0.047 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl 3-[[2-(trifluoromethyl)pyridin-4-yl]amino]benzoate | |
0.058 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl 2-[[2-(trifluoromethyl)pyridin-4-yl]amino]pyridine-3-carboxylate | |
0.064 | - |
pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl 2-{[2-(trifluoromethyl)pyridin-4-yl]amino}benzoate | |
0.26 | - |
pH 7.4, 37°C | Rattus norvegicus | (R,S)-ibuprofen | |
0.3 | - |
above, pH 7.4, 37°C | Rattus norvegicus | 4-(acetylamino)phenyl 2-[[3-(trifluoromethyl)phenyl]amino]pyridine-3-carboxylate |
General Information | Comment | Organism |
---|---|---|
physiological function | FAAH is the key hydrolytic enzyme for the endogenous cannabinoid receptor ligand anandamide | Rattus norvegicus |