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Literature summary extracted from

  • Feledziak, M.; Michaux, C.; Urbach, A.; Labar, G.; Muccioli, G.G.; Lambert, D.M.; Marchand-Brynaert, J.
    beta-Lactams derived from a carbapenem chiron are selective inhibitors of human fatty acid amide hydrolase versus human monoacylglycerol lipase (2009), J. Med. Chem., 52, 7054-7068.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.1.23 (3S)-3-[1(R)-(biphenylacetyloxy)-ethyl]-azetidin-2-one 16% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(3-phenylpropanoyl)-(3R,4R)-3-[1(R)-(3-phenylpropanoyloxy)-ethyl]-4-(acetoxy)-azetidin-2-one 100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(3-phenylpropanoyl)-(3R,4R)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-4-(acetoxy)-azetidin-2-one 100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(3-phenylpropanoyl)-(3R,4R)-3-[1(R)-(biphenylacetyloxy)-ethyl]-4-(acetoxy)-azetidin-2-one 100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0; 66% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(3-phenylpropanoyl)-(3S)-3-[1(R)-(3-phenylpropanoyloxy)-ethyl]-azetidin-2-one 100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(3-phenylpropanoyl)-(3S)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-azetidin-2-one 100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(3-phenylpropanoyl)-(3S)-3-[1(R)-(5-phenylpentanoyloxy)-ethyl]-azetidin-2-one 100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(3-phenylpropanoyl)-(3S)-3-[1(R)-(biphenylacetyloxy)-ethyl]-azetidin-2-one 31% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(4-phenylbutanoyl)-(3R,4R)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-4-(acetoxy)-azetidin-2-one 100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(4-phenylbutanoyl)-(3R,4R)-3-[1(R)-hydroxyethyl]-4-(acetoxy)-azetidin-2-one 61% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(4-phenylbutanoyl)-(3S)-3-[1(R)-(3-phenylpropanoyloxy)-ethyl]-azetidin-2-one 54% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(4-phenylbutanoyl)-(3S)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-azetidin-2-one 100% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(4-phenylbutanoyl)-(3S)-3-[1(R)-(5-phenylpentanoyloxy)-ethyl]-azetidin-2-one 59% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(5-phenylpentanoyl)-(3S)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-azetidin-2-one 39% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(5-phenylpentanoyl)-(3S)-3-[1(R)-(biphenylacetyloxy)-ethyl]-azetidin-2-one 25% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(hexa-5-enoyl)-(3S)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-azetidin-2-one 85% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(hexa-5-enoyl)-(3S)-3-[1(R)-(biphenylacetyloxy)-ethyl]-azetidin-2-one 67% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(pent-4-enoyl)-(3R,4R)-3-[1(R)-(pent-4-enoyloxy)-ethyl]-4-(acetoxy)-azetidin-2-one 99% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(pent-4-enoyl)-(3R,4R)-3-[1(R)-hydroxyethyl]-4-(acetoxy)-azetidin-2-one 16% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0; 8% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(pent-4-enoyl)-(3S)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-azetidin-2-one 89% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(pent-4-enoyl)-(3S)-3-[1(R)-(biphenylacetyloxy)-ethyl]-azetidin-2-one 91% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(pent-4-enoyl)-(3S)-3-[1(R)-(hexa-5-enoyloxy)-ethyl]-azetidin-2-one 8% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(pent-4-enoyl)-(3S)-3-[1(R)-(pent-4-enoyloxy)-ethyl]-azetidin-2-one 99% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 1-(pent-4-enoyl)-(3S)-3-[1(R)-hydroxyethyl]-azetidin-2-one 89% inhibition, with 0.1 mM of inhibitor, at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens
3.1.1.23 additional information 1-(4-phenylbutanoyl)-(3S)-3-[1(R)-hydroxyethyl]-azetidin-2-one, 1-(5-phenylpentanoyl)-(3S)-3-[1(R)-hydroxyethyl]-azetidin-2-one, 1-(hexa-5-enoyl)-(3S)-3-[1(R)-hydroxyethyl]-azetidin-2-one and 1-(4-phenylbutanoyl)-(3S)-3-[1(R)-(biphenylacetyloxy)-ethyl]-azetidin-2-one do not inhibit Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.1.1.23 Homo sapiens
-
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
3.1.1.23
-
 Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.1.23 2-oleoylglycerol + H2O
-
 Homo sapiens oleic acid + glycerol
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.1.1.23 MGL
-
 Homo sapiens
3.1.1.23 monoacylglycerol lipase
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.1.23 0.00184
-
 at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens 1-(pent-4-enoyl)-(3S)-3-[1(R)-(biphenylacetyloxy)-ethyl]-azetidin-2-one
3.1.1.23 0.00406
-
 at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens 1-(pent-4-enoyl)-(3S)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-azetidin-2-one
3.1.1.23 0.00472
-
 at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens 1-(pent-4-enoyl)-(3S)-3-[1(R)-(hexa-5-enoyloxy)-ethyl]-azetidin-2-one
3.1.1.23 0.00851
-
 at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens 1-(hexa-5-enoyl)-(3S)-3-[1(R)-(4-phenylbutanoyloxy)-ethyl]-azetidin-2-one
3.1.1.23 0.0146
-
 at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens 1-(hexa-5-enoyl)-(3S)-3-[1(R)-(biphenylacetyloxy)-ethyl]-azetidin-2-one
3.1.1.23 0.0233
-
 at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens 1-(pent-4-enoyl)-(3S)-3-[1(R)-(pent-4-enoyloxy)-ethyl]-azetidin-2-one
3.1.1.23 0.133
-
 at 37°C for 10 min, in 10 mM Tris-HCl buffer, 1 mM EDTA, 0.1% (w/v) bovine serum albumin, pH 8.0 Homo sapiens 1-(pent-4-enoyl)-(3R,4R)-3-[1(R)-(pent-4-enoyloxy)-ethyl]-4-(acetoxy)-azetidin-2-one