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Literature summary extracted from

  • Vandevoorde, S.
    Overview of the chemical families of fatty acid amide hydrolase and monoacylglycerol lipase inhibitors (2008), Curr. Top. Med. Chem., 8, 247-267.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.1.1.23 expressed in HeLa cells Rattus norvegicus

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.23 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
3.1.1.23 alpha-methyl-1-arachidonoyl glycerol compound O-1428, inhibits both cytosolic and membrane-bound MAGL Rattus norvegicus
3.1.1.23 chlorpyrifos oxon is not selective for MAGL Rattus norvegicus
3.1.1.23 ethyl octylphosphonofluoridate is not selective for MAGL Rattus norvegicus
3.1.1.23 isopropyl dodecylfluorophosphonate is not selective for MAGL Rattus norvegicus
3.1.1.23 methyl octylphosphonofluoridate is not selective for MAGL Rattus norvegicus
3.1.1.23 additional information is not inhibited by 1 mM N-arachidonylsuccinimide Rattus norvegicus
3.1.1.23 N-arachidonylmaleimide inhibits membrane-bound MAGL selectively Rattus norvegicus
3.1.1.23 S-nonylbenzodioxaphosphorin oxide is not selective for MAGL Rattus norvegicus
3.1.1.23 [1,1'-biphenyl]-3-yl-carbamic acid, cyclohexyl ester URB602, noncompetetive selective inhibitor Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.1.1.23 cytosol
-
 Rattus norvegicus 5829
-
3.1.1.23 membrane
-
 Rattus norvegicus 16020
-

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.23 Homo sapiens
-
-
-
3.1.1.23 Mus musculus
-
-
-
3.1.1.23 Rattus norvegicus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.1.1.23 brain
-
 Rattus norvegicus
-
3.1.1.23 cerebellum
-
 Rattus norvegicus
-
3.1.1.23 additional information Bv-2 cells do not express MAGL mRNA Mus musculus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.23 2-arachidonoylglycerol + H2O
-
 Rattus norvegicus arachidonic acid + glycerol
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.1.23 MAGL
-
 Mus musculus
3.1.1.23 MAGL
-
 Homo sapiens
3.1.1.23 MAGL
-
 Rattus norvegicus
3.1.1.23 monoacylglycerol lipase
-
 Mus musculus
3.1.1.23 monoacylglycerol lipase
-
 Homo sapiens
3.1.1.23 monoacylglycerol lipase
-
 Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.1.23 0.00000031
-
 cytosolic MAGL Rattus norvegicus S-nonylbenzodioxaphosphorin oxide
3.1.1.23 0.00000076
-
 cytosolic MAGL Rattus norvegicus isopropyl dodecylfluorophosphonate
3.1.1.23 0.000003
-
 cytosolic MAGL Rattus norvegicus ethyl octylphosphonofluoridate
3.1.1.23 0.000003
-
 cytosolic MAGL Rattus norvegicus methyl octylphosphonofluoridate
3.1.1.23 0.000034
-
 cytosolic MAGL Rattus norvegicus chlorpyrifos oxon
3.1.1.23 0.00014
-
 membrane-bound MAGL Rattus norvegicus N-arachidonylmaleimide
3.1.1.23 0.0002
-
 MAGL expressed in HeLa cells Rattus norvegicus 6-methyl-2-[(4-methylphenyl)amino]-4H-3,1-benzoxazin-4-one
3.1.1.23 0.01
-
 cytosolic MAGL Rattus norvegicus alpha-methyl-1-arachidonoyl glycerol
3.1.1.23 0.015
-
 cytosolic MAGL Rattus norvegicus alpha-methyl-1-arachidonoyl glycerol
3.1.1.23 0.028
-
 cytosolic MAGL Rattus norvegicus [1,1'-biphenyl]-3-yl-carbamic acid, cyclohexyl ester
3.1.1.23 0.071
-
 membrane-bound MAGL Rattus norvegicus alpha-methyl-1-arachidonoyl glycerol
3.1.1.23 0.075
-
 MAGL expressed in HeLa cells Rattus norvegicus [1,1'-biphenyl]-3-yl-carbamic acid, cyclohexyl ester