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Literature summary for 3.4.23.46 extracted from

  • Mandal, M.; Zhu, Z.; Cumming, J.N.; Liu, X.; Strickland, C.; Mazzola, R.D.; Caldwell, J.P.; Leach, P.; Grzelak, M.; Hyde, L.; Zhang, Q.; Terracina, G.; Zhang, L.; Chen, X.; Kuvelkar, R.; Kennedy, M.E.; Favreau, L.; Cox, K.; Orth, P.; Buevich, A.; Voigt, J.; Wang, H.; Kazakevich, I.; McKittrick, B.A.; Greenleew, W.; Parker, E.M.; Stamford, A.W.
    Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation (2012), J. Med. Chem., 55, 9331-9345.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
3-(5-((7aR)-6-(5-fluoropyrimidin-2-yl)-2-imino-3-methyl-4-oxooctahydro-1H-pyrrolo[3,4-d]pyrimidin-7a-yl)thiophen-3-yl)benzonitrile orally active, brain penetrant inhibitor that reduces amyloid beta40 in the plasma, cerebrospinal fluid, and cortex of rats in a dose-dependent manner Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P56817
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000004
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 3-(5-((7aR)-6-(5-fluoropyrimidin-2-yl)-2-imino-3-methyl-4-oxooctahydro-1H-pyrrolo[3,4-d]pyrimidin-7a-yl)thiophen-3-yl)benzonitrile