Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10588372 | Bioorganic & Medicinal Chemistry Letters | 2012 | 5 Pages |
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.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Angeline C.-H. Lee, Pondy Murugappan Ramanujulu, Anders Poulsen, Meredith Williams, Stéphanie Blanchard, Diana M. Ma, Zahid Bonday, Kay Lin Goh, Kee Chuan Goh, Miah Kiat Goh, Jeanette Wood, Brian W. Dymock,