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Bioorg Med Chem Lett. 2010 Mar 1;20(5):1661-4. doi: 10.1016/j.bmcl.2010.01.072. Epub 2010 Jan 21.

3-Aryl-4-(arylhydrazono)-1H-pyrazol-5-ones: Highly ligand efficient and potent inhibitors of GSK3beta.

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1
Vertex Pharmaceuticals Incorporated, 130 Waverly Street, Cambridge, MA 02139, USA.

Abstract

A series of 3-aryl-4-(arylhydrazono)-1H-pyrazol-5-one inhibitors of GSK3beta 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.

PMID:
20138514
DOI:
10.1016/j.bmcl.2010.01.072
[Indexed for MEDLINE]

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