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Literature summary for 3.1.1.23 extracted from

  • Afzal, O.; Kumar, S.; Kumar, R.; Firoz, A.; Jaggi, M.; Bawa, S.
    Docking based virtual screening and molecular dynamics study to identify potential monoacylglycerol lipase inhibitors (2014), Bioorg. Med. Chem. Lett., 24, 3986-3996.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(3R)-1-(3,4-dimethylphenyl)-5-oxo-N-[(4-oxo-3,4-dihydrophthalazin-1-yl)methyl]pyrrolidine-3-carboxamide 51.85% residual activity at 0.1 mM Homo sapiens
(3R)-N-(3,5-dimethylphenyl)-1-[2-(5-fluoro-1H-indol-3-yl)ethyl]-5-oxopyrrolidine-3-carboxamide 18.61% residual activity at 0.1 mM Homo sapiens
(3S)-N-(1,3-benzodioxol-4-ylmethyl)-1-[4-[(2-chlorobenzyl)oxy]phenyl]-5-oxopyrrolidine-3-carboxamide 51.09% residual activity at 0.1 mM Homo sapiens
1H-benzotriazol-1-yl(4-benzylpiperazin-1-yl)methanone
-
Homo sapiens
1H-benzotriazol-1-yl[4-(4-bromobenzyl)piperazin-1-yl]methanone
-
Homo sapiens
1H-benzotriazol-1-yl[4-(4-nitrobenzyl)piperazin-1-yl]methanone
-
Homo sapiens
1H-benzotriazol-1-yl[4-(naphthalen-2-ylmethyl)piperazin-1-yl]methanone
-
Homo sapiens
1H-benzotriazol-1-yl[4-[(2E)-3-phenylprop-2-en-1-yl]piperazin-1-yl]methanone
-
Homo sapiens
2-(7-methoxy-2-oxo-2H-chromen-3-yl)-N-(2-methoxyphenyl)-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxamide
-
Homo sapiens
3-[(4S)-1-[2-(5-fluoro-1H-indol-3-yl)ethyl]-2,5-dioxoimidazolidin-4-yl]-N-[(1R,2R)-2-methylcyclohexyl]propanamide 57.6% residual activity at 0.1 mM Homo sapiens
benzyl [4-(5-methoxy-2-oxo-1,3,4-oxadiazol-3(2H)-yl)-2-methylphenyl]carbamate 5.12% residual activity at 0.1 mM Homo sapiens
N-[3-(4-fluorophenyl)-6-oxopyrazolo[5,1-c]pyrido[4,3-e][1,2,4]triazin-7(6H)-yl]-2-(naphthalen-2-yloxy)acetamide 72.3% residual activity at 0.1 mM Homo sapiens
N-[4-(1,3-benzothiazol-2-yl)phenyl]-2-(1H-benzotriazol-1-yl)acetamide 14.28% residual activity at 0.1 mM Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cytosol
-
Homo sapiens 5829
-

Organism

Organism UniProt Comment Textmining
Homo sapiens Q99685
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2-arachidonoylglycerol + H2O
-
Homo sapiens glycerol + arachidonic acid
-
?

Synonyms

Synonyms Comment Organism
MAGL
-
Homo sapiens
monoacylglycerol lipase
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00001
-
pH and temperature not specified in the publication Homo sapiens N-[4-(1,3-benzothiazol-2-yl)phenyl]-2-(1H-benzotriazol-1-yl)acetamide
0.000039
-
pH and temperature not specified in the publication Homo sapiens (3R)-N-(3,5-dimethylphenyl)-1-[2-(5-fluoro-1H-indol-3-yl)ethyl]-5-oxopyrrolidine-3-carboxamide
0.000424
-
pH and temperature not specified in the publication Homo sapiens benzyl [4-(5-methoxy-2-oxo-1,3,4-oxadiazol-3(2H)-yl)-2-methylphenyl]carbamate
0.1
-
IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens 3-[(4S)-1-[2-(5-fluoro-1H-indol-3-yl)ethyl]-2,5-dioxoimidazolidin-4-yl]-N-[(1R,2R)-2-methylcyclohexyl]propanamide
0.1
-
IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens N-[3-(4-fluorophenyl)-6-oxopyrazolo[5,1-c]pyrido[4,3-e][1,2,4]triazin-7(6H)-yl]-2-(naphthalen-2-yloxy)acetamide
0.1
-
IC50 around 0.1 mM, pH and temperature not specified in the publication Homo sapiens (3S)-N-(1,3-benzodioxol-4-ylmethyl)-1-[4-[(2-chlorobenzyl)oxy]phenyl]-5-oxopyrrolidine-3-carboxamide
0.1
-
IC50 around 0.1 mM, pH and temperature not specified in the publication Homo sapiens (3R)-1-(3,4-dimethylphenyl)-5-oxo-N-[(4-oxo-3,4-dihydrophthalazin-1-yl)methyl]pyrrolidine-3-carboxamide