Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.23.46 extracted from

  • Rueeger, H.; Lueoend, R.; Rogel, O.; Rondeau, J.M.; Moebitz, H.; Machauer, R.; Jacobson, L.; Staufenbiel, M.; Desrayaud, S.; Neumann, U.
    Discovery of cyclic sulfone hydroxyethylamines as potent and selective beta-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloid beta-peptides (2013), Bioorg. Med. Chem., 23, 5300-5306.
    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
(3S,5R)-3-(4-amino-3-fluoro-5-[[(2R)-1,1,1-trifluoro-3-hydroxypropan-2-yl]oxy]benzyl)-5-[(3-tert-butylbenzyl)amino]-4-hydroxytetrahydro-2H-thiopyranium-1-olate highly potent, selective inhibitors with improved cellular activity. Sufficient central nervous system exposure can be achieved with a single oral dose of 60 micromol/kg to effect significant reduction in brain amyloid beta in APP51/16 transgenic mice Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P56817
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00001
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens (3S,5R)-3-(4-amino-3-fluoro-5-[[(2R)-1,1,1-trifluoro-3-hydroxypropan-2-yl]oxy]benzyl)-5-[(3-tert-butylbenzyl)amino]-4-hydroxytetrahydro-2H-thiopyranium-1-olate