Bioorganic and Medicinal Chemistry Letters p. 3078 - 3083 (2011)
Update date:2022-08-05
Topics:
Erlanson, Daniel A.
Arndt, Joseph W.
Cancilla, Mark T.
Cao, Kathy
Elling, Robert A.
English, Nicki
Friedman, Jessica
Hansen, Stig K.
Hession, Cathy
Joseph, Ingrid
Kumaravel, Gnanasambandam
Lee, Wen-Cherng
Lind, Ken E.
McDowell, Robert S.
Miatkowski, Konrad
Nguyen, Christine
Nguyen, Thinh B.
Park, Sophia
Pathan, Nuzhat
Penny, David M.
Romanowski, Michael J.
Scott, Daniel
Silvian, Laura
Simmons, Robert L.
Tangonan, Bradley T.
Yang, Wenjin
Sun, Lihong
We report the use of a fragment-based lead discovery method, Tethering with extenders, to discover a pyridinone fragment that binds in an adaptive site of the protein PDK1. With subsequent medicinal chemistry, this led to the discovery of a potent and hig
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