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Literature summary for 3.1.1.7 extracted from

  • Zhu, Y.; Xiao, K.; Ma, L.; Xiong, B.; Fu, Y.; Yu, H.; Wang, W.; Wang, X.; Hu, D.; Peng, H.; Li, J.; Gong, Q.; Chai, Q.; Tang, X.; Zhang, H.; Li, J.; Shen, J.
    Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and beta-secretase (2009), Bioorg. Med. Chem., 17, 1600-1613.
    View publication on PubMed
Search for more literature for 3.1.1.7

Inhibitors

Inhibitors Comment Organism Structure
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-5-nitro-N'-[(R)-1-phenylethyl]isophthalamide
-
 Homo sapiens
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-5-[methyl(methylsulfonyl)-amino]-N'-[(R)-1-(4-fluorophenyl)ethyl]isophthalamide
-
 Homo sapiens
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-5-[methyl(methylsulfonyl)amino]-N-[(R)-1-phenylethyl]isophthalamide shows inhibitory effects on beta amyloid production of amyloid precursor protein-transfected HEK293 cells and mild protective effect against hydrogen peroxide-induced cell injury Homo sapiens
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N',N'-dipropyl-5-nitroisophthalamide
-
 Homo sapiens
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N',N'-dipropyl-5-[methyl(methylsulfonyl)amino]isophthalamide
-
 Homo sapiens
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N',N'-dipropylisophthalamide
-
 Homo sapiens
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-nitroisophthalamide
-
 Homo sapiens
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-isophthalamide
-
 Homo sapiens
(1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N'-[(R)-1-phenylethyl]isophthalamide
-
 Homo sapiens
donepezil 7.9% inhibition at 0.025 mM Homo sapiens
N-((4S,5S,7R)-2-[7-(1-benzylpiperidin-4-yl)]carbamoyl-5-hydroxy-2-methyloct-4-yl)-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenyl ethyl]isophthalamide 48.7% inhibition at 0.025 mM Homo sapiens
N-((4S,5S,7R)-2-[7-(1-benzylpiperidin-4-yl)]carbamoyl-5-hydroxy-2-methyloct-4-yl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]isophthalamide 47.5% inhibition at 0.025 mM Homo sapiens
N-((4S,5S,7R)-2-[7-(1-benzylpiperidin-4-yl)]ethylcarbamoyl-5-hydroxy-2-methyloctan-4-yl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]isophthalamide 23.8% inhibition at 0.025 mM Homo sapiens
N-((4S,5S,7R)-2-[7-(1-benzylpiperidin-4-yl)]methylcarbamoyl-5-hydroxy-2-methyloct-4-yl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]isophthalamide 45.9% inhibition at 0.025 mM Homo sapiens
N-((4S,5S,7R)-2-[7-(4-benzylpiperazin-1-yl)]carbamoyl-5-hydroxy-2-methyloct-4-yl)-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide 5.2% inhibition at 0.025 mM Homo sapiens
N-([2S,3(R,S)]-2-[4-(1-benzylpiperidin-4-yl)]ethyl-carbamoyl-3-hydroxy-1-phenylbut-2-yl)-5-[methyl-(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide
-
 Homo sapiens
N-([2S,3(R,S)]-2-[4-(1-benzylpiperidin-4-yl)]ethylcarbamoyl-3-hydroxy-1-phenylbut-2-yl)-N',N'-dipropyl-5-nitroisophthalamide
-
 Homo sapiens
N-([2S,3(R,S)]-2-[4-(1-benzylpiperidin-4-yl)]ethylcarbamoyl-3-hydroxy-1-phenylbut-2-yl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]iso phthalamide
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HEK-293 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
S-acetylthiocholine + H2O detection with 5,5'-dithio-bis-2-nitrobenzoic acid, i.e. DTNB Homo sapiens acetate + thiocholine
-
 ?

Synonyms

Synonyms Comment Organism
AChE
-
 Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
 assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00105
-
 pH 8.0, 37°C Homo sapiens (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N',N'-dipropyl-5-[methyl(methylsulfonyl)amino]isophthalamide
0.00111
-
 pH 8.0, 37°C Homo sapiens N-([2S,3(R,S)]-2-[4-(1-benzylpiperidin-4-yl)]ethyl-carbamoyl-3-hydroxy-1-phenylbut-2-yl)-5-[methyl-(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide
0.00127
-
 pH 8.0, 37°C Homo sapiens (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N',N'-dipropyl-5-nitroisophthalamide
0.00135
-
 pH 8.0, 37°C Homo sapiens (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-5-[methyl(methylsulfonyl)-amino]-N'-[(R)-1-(4-fluorophenyl)ethyl]isophthalamide
0.00139
-
 pH 8.0, 37°C Homo sapiens N-([2S,3(R,S)]-2-[4-(1-benzylpiperidin-4-yl)]ethylcarbamoyl-3-hydroxy-1-phenylbut-2-yl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-[methyl(methylsulfonyl)amino]iso phthalamide
0.00168
-
 pH 8.0, 37°C Homo sapiens N-([2S,3(R,S)]-2-[4-(1-benzylpiperidin-4-yl)]ethylcarbamoyl-3-hydroxy-1-phenylbut-2-yl)-N',N'-dipropyl-5-nitroisophthalamide
0.00183
-
 pH 8.0, 37°C, in vitro AChE inhibition Homo sapiens (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-5-[methyl(methylsulfonyl)amino]-N-[(R)-1-phenylethyl]isophthalamide
0.00209
-
 pH 8.0, 37°C Homo sapiens (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-5-nitroisophthalamide
0.00228
-
 pH 8.0, 37°C Homo sapiens (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N',N'-dipropylisophthalamide
0.00253
-
 pH 8.0, 37°C Homo sapiens (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-5-nitro-N'-[(R)-1-phenylethyl]isophthalamide
0.00306
-
 pH 8.0, 37°C Homo sapiens (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N'-[(R)-1-phenylethyl]isophthalamide
0.0117
-
 pH 8.0, 37°C Homo sapiens (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-N'-[(R)-1-(4-fluorophenyl)ethyl]-isophthalamide
0.0987
-
 in vivo in amyloid precursor protein-transfected HEK293 cells Homo sapiens (1S,2R)-N-(1-benzyl-2-hydroxy-3-(S)-[2-(1-benzylpiperidin-4-yl)ethylamino]-propyl)-5-[methyl(methylsulfonyl)amino]-N-[(R)-1-phenylethyl]isophthalamide