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

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Arnost M, Pierce A, ter Haar E, Lauffer D, Madden J, Tanner K, Green J

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

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

PubMed ID

20138514 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Staurosporine	Glycogen synthase kinase-3 beta	Ki (nM)	22	N/A	N/A	Details