Bioorganic and Medicinal Chemistry Letters p. 4812 - 4819 (2015)
Update date:2022-08-05
Topics:
Egbertson, Melissa
McGaughey, Georgia B.
Pitzenberger, Steven M.
Stauffer, Shaun R.
Coburn, Craig A.
Stachel, Shawn J.
Yang, Wenjin
Barrow, James C.
Neilson, Lou Anne
McWherter, Melody
Perlow, Debra
Fahr, Bruce
Munshi, Sanjeev
Allison, Timothy J.
Holloway, Katharine
Selnick, Harold G.
Yang, Zhiqiang
Swestock, John
Simon, Adam J.
Sankaranarayanan, Sethu
Colussi, Dennis
Tugusheva, Katherine
Lai, Ming-Tain
Pietrak, Beth
Haugabook, Shari
Jin, Lixia
Chen
Holahan, Marie
Stranieri-Michener, Maria
Cook, Jacquelynn J.
Vacca, Joseph
Graham, Samuel L.
The IC50 of a beta-secretase (BACE-1) lead compound was improved ~200-fold from 11 μM to 55 nM through the addition of a single methyl group. Computational chemistry, small molecule NMR, and protein crystallography capabilities were used to com
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