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4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy

descriptionPublicationkeyboard_double_arrow_right Article 01 Aug 2012Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 22, pages 5,222-5,226 (issn: 0960-894X,

Authors: John Martin Pritchard; Rick P. C. Cousins; Mary A. Morse; Paul Faulder; John Liddle; William L. Rumsey; Chun-wa Chung; +14 Authors

doi: 10.1016/j.bmcl.2012.06.065

pmid: 22801646

4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy

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Abstract

The lead optimization of a series of potent azaindole IKK2 inhibitors is described. Optimization of the human whole blood activity and selectivity over IKK1 in parallel led to the discovery of 16, a potent and selective IKK2 inhibitor showing good efficacy in a rat model of neutrophil activation.

Related Organizations

GlaxoSmithKline (United States)
United States
Cellzome, GSK, Middlesex, UK.
GlaxoSmithKline (United Kingdom)
United Kingdom

Keywords

Indoles, Neutrophils, Biological Availability, I-kappa B Kinase, Rats, Disease Models, Animal, Structure-Activity Relationship, Animals, Humans, Lung, Protein Kinase Inhibitors, Half-Life

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BindingDB Entry 50040522: 4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.
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4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy

4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy

4 Research products, page 1 of 1

P45983

4AWI

4AWI

BindingDB Entry 50040522: 4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.