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Literature summary for 3.1.1.23 extracted from
- Overview of the chemical families of fatty acid amide hydrolase and monoacylglycerol lipase inhibitors (2008), Curr. Top. Med. Chem., 8, 247-267.
Cloned(Commentary)
| Cloned (Comment) | Organism |
|---|---|
| expressed in HeLa cells | Rattus norvegicus |
Inhibitors
| Inhibitors | Comment | Organism | Structure |
|---|---|---|---|
| 6-methyl-2-[(4-methylphenyl)amino]-4H-3,1-benzoxazin-4-one | URB754, inhibition of brain MAGL expressed in HeLa cells, no inhibition of membrane-bound MAGL. Is not selective for MAGL | Rattus norvegicus |  |
| alpha-methyl-1-arachidonoyl glycerol | compound O-1428, inhibits both cytosolic and membrane-bound MAGL | Rattus norvegicus | |
| chlorpyrifos oxon | is not selective for MAGL | Rattus norvegicus | |
| ethyl octylphosphonofluoridate | is not selective for MAGL | Rattus norvegicus | |
| isopropyl dodecylfluorophosphonate | is not selective for MAGL | Rattus norvegicus | |
| methyl octylphosphonofluoridate | is not selective for MAGL | Rattus norvegicus | |
| additional information | is not inhibited by 1 mM N-arachidonylsuccinimide | Rattus norvegicus | |
| N-arachidonylmaleimide | inhibits membrane-bound MAGL selectively | Rattus norvegicus | |
| S-nonylbenzodioxaphosphorin oxide | is not selective for MAGL | Rattus norvegicus | |
| [1,1'-biphenyl]-3-yl-carbamic acid, cyclohexyl ester | URB602, noncompetetive selective inhibitor | Rattus norvegicus | |
Localization
| Localization | Comment | Organism | GeneOntology No. | Textmining |
|---|---|---|---|---|
| cytosol | - |
Rattus norvegicus | 5829 | - |
| membrane | - |
Rattus norvegicus | 16020 | - |
Organism
| Organism | UniProt | Comment | Textmining |
|---|---|---|---|
| Homo sapiens | - |
- |
- |
| Mus musculus | - |
- |
- |
| Rattus norvegicus | - |
- |
- |
Source Tissue
| Source Tissue | Comment | Organism | Textmining |
|---|---|---|---|
| brain | - |
Rattus norvegicus | - |
| cerebellum | - |
Rattus norvegicus | - |
| additional information | Bv-2 cells do not express MAGL mRNA | Mus musculus | - |
Substrates and Products (Substrate)
| Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
|---|---|---|---|---|---|---|
| 2-arachidonoylglycerol + H2O | - |
Rattus norvegicus | arachidonic acid + glycerol | - |
? | |
Synonyms
| Synonyms | Comment | Organism |
|---|---|---|
| MAGL | - |
Mus musculus |
| MAGL | - |
Homo sapiens |
| MAGL | - |
Rattus norvegicus |
| monoacylglycerol lipase | - |
Mus musculus |
| monoacylglycerol lipase | - |
Homo sapiens |
| monoacylglycerol lipase | - |
Rattus norvegicus |
IC50 Value
| IC50 Value | IC50 Value Maximum | Comment | Organism | Inhibitor | Structure |
|---|---|---|---|---|---|
| 0.00000031 | - |
cytosolic MAGL | Rattus norvegicus | S-nonylbenzodioxaphosphorin oxide | |
| 0.00000076 | - |
cytosolic MAGL | Rattus norvegicus | isopropyl dodecylfluorophosphonate | |
| 0.000003 | - |
cytosolic MAGL | Rattus norvegicus | ethyl octylphosphonofluoridate | |
| 0.000003 | - |
cytosolic MAGL | Rattus norvegicus | methyl octylphosphonofluoridate | |
| 0.000034 | - |
cytosolic MAGL | Rattus norvegicus | chlorpyrifos oxon | |
| 0.00014 | - |
membrane-bound MAGL | Rattus norvegicus | N-arachidonylmaleimide | |
| 0.0002 | - |
MAGL expressed in HeLa cells | Rattus norvegicus | 6-methyl-2-[(4-methylphenyl)amino]-4H-3,1-benzoxazin-4-one | |
| 0.01 | - |
cytosolic MAGL | Rattus norvegicus | alpha-methyl-1-arachidonoyl glycerol | |
| 0.015 | - |
cytosolic MAGL | Rattus norvegicus | alpha-methyl-1-arachidonoyl glycerol | |
| 0.028 | - |
cytosolic MAGL | Rattus norvegicus | [1,1'-biphenyl]-3-yl-carbamic acid, cyclohexyl ester | |
| 0.071 | - |
membrane-bound MAGL | Rattus norvegicus | alpha-methyl-1-arachidonoyl glycerol | |
| 0.075 | - |
MAGL expressed in HeLa cells | Rattus norvegicus | [1,1'-biphenyl]-3-yl-carbamic acid, cyclohexyl ester | |
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Release 2023.1 (January 2023)
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