| Literature DB >> 19409780 |
Shawn J Stachel1, Craig A Coburn, Diane Rush, Kristen L G Jones, Hong Zhu, Hemaka Rajapakse, Samuel L Graham, Adam Simon, M Katharine Holloway, Tim J Allison, Sanjeev K Munshi, Amy S Espeseth, Paul Zuck, Dennis Colussi, Abigail Wolfe, Beth L Pietrak, Ming-Tain Lai, Joseph P Vacca.
Abstract
We have developed a novel series of heteroaromatic BACE-1 inhibitors. These inhibitors interact with the enzyme in a unique fashion that allows for potent binding in a non-traditional paradigm. In addition to the elucidation of their binding profile, we have discovered a pH dependent effect on the binding affinity as a result of the intrinsic pK(a) of these inhibitors and the pH of the BACE-1 enzyme binding assay.Entities:
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Year: 2009 PMID： 19409780 DOI： 10.1016/j.bmcl.2009.04.033
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823