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Literature summary for 3.5.1.99 extracted from

  • Sundermann, T.; Hanekamp, W.; Lehr, M.
    Structure-activity relationship studies on 1-heteroaryl-3-phenoxypropan-2-ones acting as inhibitors of cytosolic phospholipase A2alpha and fatty acid amide hydrolase replacement of the activated ketone group by other serine traps (2016), J. Enzyme Inhib. Med. Chem., 31, 653-663 .
    View publication on PubMed
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Application

Application Comment Organism
medicine inhibitors of fatty acid amide hydrolase may represent new drug candidates for the treatment of inflammation Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(1H-benzotriazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one
-
 Homo sapiens
1-(4-phenoxyphenoxy)-3-(2H-tetrazol-2-yl)propan-2-one
-
 Homo sapiens
2-(1H-benzotriazol-1-yl)-1-(5-phenoxy-1,3-benzoxazol-2-yl)ethan-1-one
-
 Homo sapiens
additional information the replacement of the activated ketone functionality of the fatty acid amide hydrolase inhibitors 1-(1H-benzotriazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one and 1-(4-phenoxyphenoxy)-3-(2H-tetrazol-2-yl)propan-2-one, by a-ketoheterocycle, cyanamide, and nitrile is not well tolerated. The resulting compounds are only weakly or even not active against the enzyme Homo sapiens
[1-(4-phenoxyphenoxy)-3-(2H-tetrazol-2-yl)propan-2-yl]cyanamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-(2-hydroxyethyl)-4-pyren-1-ylbutanamide + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
FAAH
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000008
-
 pH and temperature not specified in the publication Homo sapiens 1-(4-phenoxyphenoxy)-3-(2H-tetrazol-2-yl)propan-2-one
0.000024
-
 pH and temperature not specified in the publication Homo sapiens 1-(1H-benzotriazol-1-yl)-3-(4-phenoxyphenoxy)propan-2-one
0.0053
-
 pH and temperature not specified in the publication Homo sapiens [1-(4-phenoxyphenoxy)-3-(2H-tetrazol-2-yl)propan-2-yl]cyanamide
0.01
-
 pH and temperature not specified in the publication Homo sapiens 2-(1H-benzotriazol-1-yl)-1-(5-phenoxy-1,3-benzoxazol-2-yl)ethan-1-one

General Information

General Information Comment Organism
physiological function terminates the anti-inflammatory effects of endocannabinoids Homo sapiens