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Bioorg Med Chem Lett
; 22(12): 4023-7, 2012 Jun 15.
Artículo
en Inglés
| MEDLINE
| ID: mdl-22591730
RESUMEN
Ligand efficient fragments binding to PDK1 were identified by an NMR fragment-based screening approach. Computational modeling of the fragments bound to the active site led to the design and synthesis of a series of novel 6,7-disubstituted thienopyrimidin-4-one compounds, with low micromolar inhibitory activity against PDK1 in a biochemical enzyme assay.