1.
Bioorg Med Chem Lett
; 21(10): 3078-83, 2011 May 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21459573
RESUMO
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 highly selective inhibitor of PDK1, which binds in the 'DFG-out' conformation.