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Literature summary for 3.4.23.46 extracted from

  • Thomas, A.A.; Hunt, K.W.; Newhouse, B.; Watts, R.J.; Liu, X.; Vigers, G.; Smith, D.; Rhodes, S.P.; Brown, K.D.; Otten, J.N.; Burkard, M.; Cox, A.A.; Geck Do, M.K.; Dutcher, D.; Rana, S.; DeLisle, R.K.; Regal, K.; Wright, A.D.; Groneberg, R.; Liao, J.; Scearce-Levie, K.; Siu, M.; Purkey, H.E.; Lyssikatos, J.P.
    8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors (2014), J. Med. Chem., 57, 10112-10129.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in CHO cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(4aS,4'S,10aR)-8-(2-fluoropyridin-3-yl)-4a-methyl-3,4,4a,10a-tetrahydro-2H,5'H-spiro[pyrano[3,2-b]chromene-10,4'-thiazol]-2'-amine compound demonstrates a 69% reduction in rat cerebrospinal fluid amyloid beta1?40 at 60 mg/kg Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P56817
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000045
-
pH 4.4, 22°C Homo sapiens (4aS,4'S,10aR)-8-(2-fluoropyridin-3-yl)-4a-methyl-3,4,4a,10a-tetrahydro-2H,5'H-spiro[pyrano[3,2-b]chromene-10,4'-thiazol]-2'-amine