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Literature summary extracted from
- Mechanism of inhibition of fatty acid amide hydrolase by sulfonamide-containing benzothiazoles: long residence time derived from increased kinetic barrier and not exclusively from thermodynamic potency (2011), Biochemistry, 50, 6867-6878.
Cloned(Commentary)
| EC Number | Cloned (Comment) | Organism |
|---|---|---|
| 3.5.1.99 | expression of humanized rat FAAH | Rattus norvegicus |
| 3.5.1.99 | stable expression of FAAH in CHO cells | Homo sapiens |
Protein Variants
| EC Number | Protein Variants | Comment | Organism |
|---|---|---|---|
| 3.5.1.99 | additional information | generation of humanized rat FAAH | Homo sapiens |
Inhibitors
| EC Number | Inhibitors | Comment | Organism | Structure |
|---|---|---|---|---|
| 3.5.1.99 | 7-phenyl-1-[5-(pyridin-2-yl)-1,3-oxazol-2-yl]heptan-1-one | OL-135, an alpha-keto-heterocycle that is a covalent reversible inhibitor of FAAH | Homo sapiens |  |
| 3.5.1.99 | 7-phenyl-1-[5-(pyridin-2-yl)-1,3-oxazol-2-yl]heptan-1-one | OL-135, an alpha-keto-heterocycle that is a covalent reversible inhibitor of FAAH | Rattus norvegicus | |
| 3.5.1.99 | additional information | mechanism of inhibition of fatty acid amide hydrolase by sulfonamide-containing benzothiazoles, long residence time derived from increased kinetic barrier and not exclusively from thermodynamic potency, transition-state analogues, overview | Homo sapiens | |
| 3.5.1.99 | additional information | mechanism of inhibition of fatty acid amide hydrolase by sulfonamide-containing benzothiazoles, long residence time derived from increased kinetic barrier and not exclusively from thermodynamic potency, transition-state analogues, overview | Rattus norvegicus | |
| 3.5.1.99 | N-[4-(4-methoxy-1,3-benzothiazol-2-yl)phenyl]-1-(thiophen-2-ylsulfonyl)piperidine-4-carboxamide | a reversible, albeit slowly dissociating inhibitor of FAAH, reversibly and noncovalently inhibiting, molecular docking and computational modeling of interactions of the benzothiazole analogue 1 with humanized rat FAAH by induced fit docking, overview. Failure to observe the formation of covalent enzyme-inhibitor adduct or putative cleavage product using electrospray mass spectrometric techniques | Homo sapiens | |
| 3.5.1.99 | N-[4-(4-methoxy-1,3-benzothiazol-2-yl)phenyl]-1-(thiophen-2-ylsulfonyl)piperidine-4-carboxamide | a reversible, albeit slowly dissociating inhibitor of FAAH, reversibly and noncovalently inhibiting, molecular docking and computational modeling of interactions of the benzothiazole analogue 1 with humanized rat FAAH by induced fit docking, overview. Failure to observe the formation of covalent enzyme-inhibitor adduct or putative cleavage product using electrospray mass spectrometric techniques | Rattus norvegicus | |
| 3.5.1.99 | URB597 | a carbamate inhibiting FAAH covalently and irreversibly, time-dependent inhibition, overview | Homo sapiens | |
| 3.5.1.99 | URB597 | a carbamate inhibiting FAAH covalently and irreversibly, time-dependent inhibition, overview | 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 | Homo sapiens | i.e. arachidonoyl ethanolamide | arachidonic acid + ethanolamine | - |
? | |
| 3.5.1.99 | anandamide + H2O | Rattus norvegicus | i.e. arachidonoyl ethanolamide | arachidonic acid + ethanolamine | - |
? | |
Organism
| EC Number | Organism | UniProt | Comment | Textmining |
|---|---|---|---|---|
| 3.5.1.99 | Homo sapiens | - |
- |
- |
| 3.5.1.99 | Rattus norvegicus | - |
- |
- |
Substrates and Products (Substrate)
| EC Number | Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|---|
| 3.5.1.99 | anandamide + H2O | i.e. arachidonoyl ethanolamide | Homo sapiens | arachidonic acid + ethanolamine | - |
? | |
| 3.5.1.99 | anandamide + H2O | i.e. arachidonoyl ethanolamide | Rattus norvegicus | arachidonic acid + ethanolamine | - |
? | |
| 3.5.1.99 | decanoyl 7-amido-4-methylcoumarin + H2O | - |
Homo sapiens | ? | - |
? | |
| 3.5.1.99 | decanoyl 7-amido-4-methylcoumarin + H2O | - |
Rattus norvegicus | ? | - |
? | |
Synonyms
| EC Number | Synonyms | Comment | Organism |
|---|---|---|---|
| 3.5.1.99 | FAAH | - |
Homo sapiens |
| 3.5.1.99 | FAAH | - |
Rattus norvegicus |
Temperature Optimum [°C]
| EC Number | Temperature Optimum [°C] | Temperature Optimum Maximum [°C] | Comment | Organism |
|---|---|---|---|---|
| 3.5.1.99 | 22 | - |
assay at room temperature | Homo sapiens |
| 3.5.1.99 | 22 | - |
assay at room temperature | Rattus norvegicus |
pH Optimum
| EC Number | pH Optimum Minimum | pH Optimum Maximum | Comment | Organism |
|---|---|---|---|---|
| 3.5.1.99 | 8 | - |
assay at | Homo sapiens |
| 3.5.1.99 | 8 | - |
assay at | Rattus norvegicus |
Ki Value [mM]
| EC Number | Ki Value [mM] | Ki Value maximum [mM] | Inhibitor | Comment | Organism | Structure |
|---|---|---|---|---|---|---|
| 3.5.1.99 | additional information | - |
additional information | time-dependent inhibition kinetics with N-[4-(4-methoxy-1,3-benzothiazol-2-yl)phenyl]-1-(thiophen-2-ylsulfonyl)piperidine-4-carboxamide, recombinant enzyme not purified, detailed overview | Homo sapiens | |
| 3.5.1.99 | additional information | - |
additional information | time-dependent inhibition kinetics with N-[4-(4-methoxy-1,3-benzothiazol-2-yl)phenyl]-1-(thiophen-2-ylsulfonyl)piperidine-4-carboxamide, recombinant enzyme not purified, detailed overview | Rattus norvegicus |
IC50 Value
| EC Number | IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|---|
| 3.5.1.99 | 0.000002 | - |
pH 8.0, 22°C, at 78 nM substrate anandamide | Homo sapiens | N-[4-(4-methoxy-1,3-benzothiazol-2-yl)phenyl]-1-(thiophen-2-ylsulfonyl)piperidine-4-carboxamide | |
| 3.5.1.99 | 0.000002 | - |
pH 8.0, 22°C, at 78 nM substrate anandamide | Rattus norvegicus | N-[4-(4-methoxy-1,3-benzothiazol-2-yl)phenyl]-1-(thiophen-2-ylsulfonyl)piperidine-4-carboxamide | |
| 3.5.1.99 | 0.0000038 | - |
pH 8.0, 22°C, at 0.01 mM substrate anandamide | Homo sapiens | N-[4-(4-methoxy-1,3-benzothiazol-2-yl)phenyl]-1-(thiophen-2-ylsulfonyl)piperidine-4-carboxamide | |
| 3.5.1.99 | 0.0000038 | - |
pH 8.0, 22°C, at 0.01 mM substrate anandamide | Rattus norvegicus | N-[4-(4-methoxy-1,3-benzothiazol-2-yl)phenyl]-1-(thiophen-2-ylsulfonyl)piperidine-4-carboxamide | |
| 3.5.1.99 | 0.0000051 | - |
pH 8.0, 22°C, at 0.005 mM substrate anandamide | Homo sapiens | N-[4-(4-methoxy-1,3-benzothiazol-2-yl)phenyl]-1-(thiophen-2-ylsulfonyl)piperidine-4-carboxamide | |
| 3.5.1.99 | 0.0000051 | - |
pH 8.0, 22°C, at 0.005 mM substrate anandamide | Rattus norvegicus | N-[4-(4-methoxy-1,3-benzothiazol-2-yl)phenyl]-1-(thiophen-2-ylsulfonyl)piperidine-4-carboxamide | |
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