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Literature summary for 3.4.23.46 extracted from

  • Cheng, Y.; Judd, T.C.; Bartberger, M.D.; Brown, J.; Chen, K.; Fremeau, R.T.; Hickman, D.; Hitchcock, S.A.; Jordan, B.; Li, V.; Lopez, P.; Louie, S.W.; Luo, Y.; Michelsen, K.; Nixey, T.; Powers, T.S.; Rattan, C.; Sickmier, E.A.; St Jean, D.J.; Wahl, R.C.; Wen, P.H.; Wood, S.
    From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) (2011), J. Med. Chem., 54, 5836-5857.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
-
Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(R)-3-(2-amino-6-(3-chloropyridin-2-yl)quinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide EC50 value for cell assay 80 nM Homo sapiens
(R)-3-(2-amino-6-(3-methylpyridin-2-yl)quinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide EC50 value for cell assay 35 nM Homo sapiens
3-(6-(2-acetylphenyl)-2-aminoquinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide EC50 value for cell assay 11 nM Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000011
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens (R)-3-(2-amino-6-(3-chloropyridin-2-yl)quinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide
0.000016
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens (R)-3-(2-amino-6-(3-methylpyridin-2-yl)quinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide
0.00005
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-(6-(2-acetylphenyl)-2-aminoquinolin-3-yl)-N-(3,3-dimethylbutyl)-2-methylpropanamide