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Literature summary for 3.4.23.46 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 3.4.23.46

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(1S,2R)-N-[1-benzyl-2-hydroxy-3-(S)-[(1-benzylpiperidin-4-yl)amino]-propyl]-5-[methyl(methylsulfonyl)amino]-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 dual inhibitor of both beta-secretase and acetylcholinesterase, good inhibitory effects on amyloid beta production of 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 dual inhibitor of both beta-secretase and acetylcholinesterase. Intracerebroventricular injection of into amyloid precursor protein transgenic mice causes a 29% reduction of amyloid beta1-40 production Mus musculus
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
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Mus musculus
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
DABCYL-Ser-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-EDANS + H2O
-
 Mus musculus ?
-
 ?
DABCYL-Ser-Glu-Val-Asn-Leu-Asp-Ala-Glu-Phe-EDANS + H2O
-
 Homo sapiens ?
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000222
-
 pH 4.0 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
0.000511
-
 pH 4.0 Homo sapiens (1S,2R)-N-[1-benzyl-2-hydroxy-3-(S)-[(1-benzylpiperidin-4-yl)amino]-propyl]-5-[methyl(methylsulfonyl)amino]-N'-[(R)-1-phenylethyl]isophthalamide
0.000567
-
 pH 4.0 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
0.000616
-
 pH 4.0 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