Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 5, Pages 1661-1664Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.01.072
Keywords
GSK3 beta; Kinase inhibitors; Pyrazolones; Ligand efficiency; Binding efficiency; Hit-to-lead; Lead-like
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A series of 3-aryl-4-(arylhydrazono)-1H-pyrazol-5-one inhibitors of GSK3 beta was developed from a low molecular weight, highly ligand efficient screening hit 1. Hit-to-lead optimization led to a number of highly potent inhibitors, while maintaining the high ligand efficiency of the screening hit. (C) 2010 Elsevier Ltd. All rights reserved.
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