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Literature summary for 3.5.1.99 extracted from

  • Deplano, A.; Morgillo, C.M.; Demurtas, M.; Bjoerklund, E.; Cipriano, M.; Svensson, M.; Hashemian, S.; Smaldone, G.; Pedone, E.; Luque, F.J.; Cabiddu, M.G.; Novellino, E.; Fowler, C.J.; Catalanotti, B.; Onnis, V.
    Novel propanamides as fatty acid amide hydrolase inhibitors (2017), Eur. J. Med. Chem., 136, 523-542 .
    View publication on PubMed
Search for more literature for 3.5.1.99

Inhibitors

Inhibitors Comment Organism Structure
2-methyl-N-(3-methylpyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
additional information FAAH inhibition represents a promising strategy to activate the cannabinoid system, since it does not result in the psychotropic and peripheral side effects characterizing the agonists of the cannabinoid receptors Rattus norvegicus
N-(1,4-dihydroquinolin-8-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-(2-methylphenyl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-(3-bromopyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-(3-chloropyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-(3-iodopyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-(3-methylpyridin-2-yl)-1-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)cyclobutane-1-carboxamide
-
 Rattus norvegicus
N-(3-methylpyridin-2-yl)-1-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)cyclohexane-1-carboxamide 30% inhibition at 0.1 mM Rattus norvegicus
N-(3-methylpyridin-2-yl)-1-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)cyclopentane-1-carboxamide
-
 Rattus norvegicus
N-(3-methylpyridin-2-yl)-1-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)cyclopropane-1-carboxamide
-
 Rattus norvegicus
N-(3-methylpyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)acetamide
-
 Rattus norvegicus
N-(3-methylpyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-(3-methylpyridin-2-yl)-2-(4-[[7-(trifluoromethyl)quinolin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-(3-methylpyridin-2-yl)-2-(4-[[8-(trifluoromethyl)quinolin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-(4-methylpyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-(5-methylpyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-(pyrazin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-(pyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-(pyridin-3-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-(pyridin-4-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-(pyrimidin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-[(pyridin-2-yl)methyl]-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-[(pyridin-3-yl)methyl]-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-[2-[(3-methylpyridin-2-yl)amino]-2-oxoethyl]-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-[3-(trifluoromethyl)pyridin-2-yl]-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus
N-[4-(2,3-dimethylphenyl)piperazin-1-yl]-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide 24% inhibition at 0.1 mM Rattus norvegicus
N-[4-(2-methylphenyl)piperazin-1-yl]-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide 24% inhibition at 0.1 mM Rattus norvegicus
N-[4-(4-chlorophenyl)piperazin-1-yl]-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
-
 Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus P97612
-
-

Source Tissue

Source Tissue Comment Organism Textmining
brain
-
 Rattus norvegicus
-

Synonyms

Synonyms Comment Organism
FAAH
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000058
-
 37°C, pH 7.4 Rattus norvegicus N-(3-chloropyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.00013
-
 37°C, pH 7.4 Rattus norvegicus N-(3-bromopyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.00013
-
 37°C, pH 7.4 Rattus norvegicus N-(3-iodopyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.00033
-
 37°C, pH 7.4 Rattus norvegicus N-[3-(trifluoromethyl)pyridin-2-yl]-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.00059
-
 37°C, pH 7.4 Rattus norvegicus N-(3-methylpyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.00074
-
 37°C, pH 7.4 Rattus norvegicus N-(2-methylphenyl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.00099
-
 37°C, pH 7.4 Rattus norvegicus N-(pyrimidin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.0018
-
 37°C, pH 7.4 Rattus norvegicus 2-methyl-N-(3-methylpyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.002
-
 37°C, pH 7.4 Rattus norvegicus N-(pyrazin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.0024
-
 37°C, pH 7.4 Rattus norvegicus N-[2-[(3-methylpyridin-2-yl)amino]-2-oxoethyl]-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.0031
-
 37°C, pH 7.4 Rattus norvegicus N-(3-methylpyridin-2-yl)-2-(4-[[7-(trifluoromethyl)quinolin-4-yl]amino]phenyl)propanamide
0.004
-
 37°C, pH 7.4 Rattus norvegicus N-(4-methylpyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.0043
-
 37°C, pH 7.4 Rattus norvegicus N-(1,4-dihydroquinolin-8-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.0064
-
 37°C, pH 7.4 Rattus norvegicus N-(pyridin-3-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.0091
-
 37°C, pH 7.4 Rattus norvegicus N-(3-methylpyridin-2-yl)-1-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)cyclobutane-1-carboxamide
0.011
-
 37°C, pH 7.4 Rattus norvegicus N-(5-methylpyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.012
-
 37°C, pH 7.4 Rattus norvegicus N-(pyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.014
-
 37°C, pH 7.4 Rattus norvegicus N-(3-methylpyridin-2-yl)-1-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)cyclopropane-1-carboxamide
0.017
-
 37°C, pH 7.4 Rattus norvegicus N-[4-(4-chlorophenyl)piperazin-1-yl]-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.023
-
 37°C, pH 7.4 Rattus norvegicus N-[(pyridin-2-yl)methyl]-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.027
-
 37°C, pH 7.4 Rattus norvegicus N-(3-methylpyridin-2-yl)-2-(4-[[8-(trifluoromethyl)quinolin-4-yl]amino]phenyl)propanamide
0.027
-
 37°C, pH 7.4 Rattus norvegicus N-[2-[(3-methylpyridin-2-yl)amino]-2-oxoethyl]-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.032
-
 37°C, pH 7.4 Rattus norvegicus N-[(pyridin-3-yl)methyl]-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.048
-
 37°C, pH 7.4 Rattus norvegicus N-(3-methylpyridin-2-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)acetamide
0.052
-
 37°C, pH 7.4 Rattus norvegicus N-(pyridin-4-yl)-2-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)propanamide
0.06
-
 37°C, pH 7.4 Rattus norvegicus N-(3-methylpyridin-2-yl)-1-(4-[[2-(trifluoromethyl)pyridin-4-yl]amino]phenyl)cyclopentane-1-carboxamide

General Information

General Information Comment Organism
metabolism the enzyme has a key role in the control of the cannabinoid signaling, through the hydrolysis of the endocannabinoids anandamide and in some tissues 2-arachidonoylglycerol Rattus norvegicus