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Literature summary for 3.5.1.99 extracted from

  • Deplano, A.; Cipriano, M.; Moraca, F.; Novellino, E.; Catalanotti, B.; Fowler, C.J.; Onnis, V.
    Benzylamides and piperazinoarylamides of ibuprofen as fatty acid amide hydrolase inhibitors (2019), J. Enzyme Inhib. Med. Chem., 34, 562-576 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.5.1.99

Application

Application Comment Organism
medicine inhibition of fatty acid amide hydrolasis is considered a powerful approach to enhance the endocannabinoid signalling and is a potential target for the treatment of neurological disorders such as anxiety or depression, or of inflammatory process Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
1,1,1-trifluoro-N-([1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamoyl)methanesulfonamide
-
 Rattus norvegicus
1-(4-benzylpiperazin-1-yl)-2-[4-(2-methylpropyl)phenyl]propan-1-one 18% inhibition at 0.1 mM Rattus norvegicus
1-[4-(2,3-dimethylphenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one
-
 Rattus norvegicus
1-[4-(2-methylphenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one 33% inhibition at 0.1 mM Rattus norvegicus
1-[4-(3,4-dichlorophenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one
-
 Rattus norvegicus
1-[4-(3-chlorophenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one
-
 Rattus norvegicus
1-[4-(3-methoxyphenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one 41% inhibition at 0.1 mM Rattus norvegicus
1-[4-(3-methylphenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one
-
 Rattus norvegicus
1-[4-(4-chlorophenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one
-
 Rattus norvegicus
1-[4-(4-fluorophenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one
-
 Rattus norvegicus
1-[4-(4-methoxyphenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one
-
 Rattus norvegicus
1-[4-[(3-chlorophenyl)methyl]piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one 8% inhibition at 0.1 mM Rattus norvegicus
2-[4-(2-methylpropyl)phenyl]-1-(4-phenylpiperazin-1-yl)propan-1-one
-
 Rattus norvegicus
2-[4-(2-methylpropyl)phenyl]-N-(3-methylpyridin-2-yl)propanamide
-
 Rattus norvegicus
2-[4-(2-methylpropyl)phenyl]-N-[[3-(trifluoromethyl)phenyl]methyl]propanamide
-
 Rattus norvegicus
2-[4-(2-methylpropyl)phenyl]-N-[[4-(trifluoromethyl)phenyl]methyl]propanamide
-
 Rattus norvegicus
N-([1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamoyl)benzenesulfonamide
-
 Rattus norvegicus
N-([1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamoyl)methanesulfonamide
-
 Rattus norvegicus
N-[(2,4-dichlorophenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide
-
 Rattus norvegicus
N-[(2,5-dichlorophenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide
-
 Rattus norvegicus
N-[(2,6-dichlorophenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide 19% inhibition at 0.1 mM Rattus norvegicus
N-[(2-chlorophenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide
-
 Rattus norvegicus
N-[(2-methoxyphenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide
-
 Rattus norvegicus
N-[(3,4-dichlorophenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide
-
 Rattus norvegicus
N-[(3-hydroxy-4-methoxyphenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide
-
 Rattus norvegicus
N-[(4-methoxyphenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide
-
 Rattus norvegicus
N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]-N'-phenylurea
-
 Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus P97612
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
N-arachidonoylethanolamine + H2O
-
 Rattus norvegicus arachidonic acid + ethanolamine
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0017
-
 37°C, pH 7.4 Rattus norvegicus 1-[4-(2,3-dimethylphenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one
0.0017
-
 37°C, pH 7.4 Rattus norvegicus 1-[4-(3-chlorophenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one
0.0017
-
 37°C, pH 7.4 Rattus norvegicus 1-[4-(4-chlorophenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one
0.0041
-
 37°C, pH 7.4 Rattus norvegicus N-[(2-chlorophenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide
0.0044
-
 37°C, pH 7.4 Rattus norvegicus N-[(2,5-dichlorophenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide
0.0045
-
 37°C, pH 7.4 Rattus norvegicus 1-[4-(4-methoxyphenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one
0.0047
-
 37°C, pH 7.4 Rattus norvegicus 2-[4-(2-methylpropyl)phenyl]-1-(4-phenylpiperazin-1-yl)propan-1-one
0.0052
-
 37°C, pH 7.4 Rattus norvegicus 2-[4-(2-methylpropyl)phenyl]-N-(3-methylpyridin-2-yl)propanamide
0.016
-
 37°C, pH 7.4 Rattus norvegicus 1-[4-(3,4-dichlorophenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one
0.016
-
 37°C, pH 7.4 Rattus norvegicus 1-[4-(3-methylphenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one
0.017
-
 37°C, pH 7.4 Rattus norvegicus 1-[4-(4-fluorophenyl)piperazin-1-yl]-2-[4-(2-methylpropyl)phenyl]propan-1-one
0.018
-
 37°C, pH 7.4 Rattus norvegicus N-[(2-methoxyphenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide
0.018
-
 37°C, pH 7.4 Rattus norvegicus N-[(3-hydroxy-4-methoxyphenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide
0.021
-
 37°C, pH 7.4 Rattus norvegicus N-[(2,4-dichlorophenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide
0.021
-
 37°C, pH 7.4 Rattus norvegicus N-[1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]-N'-phenylurea
0.025
-
 37°C, pH 7.4 Rattus norvegicus 1,1,1-trifluoro-N-([1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamoyl)methanesulfonamide
0.027
-
 37°C, pH 7.4 Rattus norvegicus N-([1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamoyl)benzenesulfonamide
0.027
-
 37°C, pH 7.4 Rattus norvegicus N-([1-[2-oxo-3-(4-phenoxyphenoxy)propyl]-1H-indazol-5-yl]carbamoyl)methanesulfonamide
0.028
-
 37°C, pH 7.4 Rattus norvegicus 2-[4-(2-methylpropyl)phenyl]-N-[[3-(trifluoromethyl)phenyl]methyl]propanamide
0.036
-
 37°C, pH 7.4 Rattus norvegicus N-[(3,4-dichlorophenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide
0.043
-
 37°C, pH 7.4 Rattus norvegicus N-[(4-methoxyphenyl)methyl]-2-[4-(2-methylpropyl)phenyl]propanamide
0.051
-
 37°C, pH 7.4 Rattus norvegicus 2-[4-(2-methylpropyl)phenyl]-N-[[4-(trifluoromethyl)phenyl]methyl]propanamide

General Information

General Information Comment Organism
physiological function the enzyme plays a key role in controlling endogenous levels of endocannabinoids Rattus norvegicus