Discovery of a potent and highly selective PDK1 inhibitor via fragment-based drug discovery.
2011
Abstract We report the use of a
fragment-based lead discoverymethod,
Tetheringwith extenders, to discover a pyridinone fragment that binds in an adaptive site of the protein PDK1. With subsequent
medicinal chemistry, this led to the
discoveryof a potent and highly selective inhibitor of PDK1, which binds in the ‘DFG-out’ conformation.
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