Article ID Journal Published Year Pages File Type
10588372 Bioorganic & Medicinal Chemistry Letters 2012 5 Pages PDF
Abstract
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.
Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
Authors
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