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

BRENDA support

Literature summary for 3.4.23.46 extracted from

  • Butler, C.R.; Brodney, M.A.; Beck, E.M.; Barreiro, G.; Nolan, C.E.; Pan, F.; Vajdos, F.; Parris, K.; Varghese, A.H.; Helal, C.J.; Lira, R.; Doran, S.D.; Riddell, D.R.; Buzon, L.M.; Dutra, J.K.; Martinez-Alsina, L.A.; Ogilvie, K.; Murray, J.C.; Young, J.M.; Atchison, K.; Robshaw, A.; Gonzales, C.; Wang, J.; Zhang, Y.; O'Neill, B.T.
    Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design (2015), J. Med. Chem., 58, 2678-2702.
    View publication on PubMed
Search for more literature for 3.4.23.46

Inhibitors

Inhibitors Comment Organism Structure
(4aR,6R,8aS)-8a-(2,4-difluorophenyl)-6-(fluoromethyl)-4,4a,5,6,8,8a-hexahydropyrano[3,4-d][1,3]thiazin-2-amine upon oral administration, inhibitor exhibits robust brain availability and is efficacious in lowering central amyloid beta levels in mouse and dog. Chronic treatment in aged PS1/APP mice effects a decrease in the number and size of amyloid-beta-derived plaques. Evaluation of the inhibitor in a 2-week exploratory toxicology study exhibits no accumulation of autofluorescent material in retinal pigment epithelium or histology findings in the eye Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P56817
-
-

Source Tissue

Source Tissue Comment Organism Textmining
H4 neuroglioma cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
biotin-GLTNIKTEEISEISYEVEFR-C[Oregon Green]-KK-OH + H2O
-
 Homo sapiens ?
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00107
-
 pH 4.5, 37°C Homo sapiens (4aR,6R,8aS)-8a-(2,4-difluorophenyl)-6-(fluoromethyl)-4,4a,5,6,8,8a-hexahydropyrano[3,4-d][1,3]thiazin-2-amine