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4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy |
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| Authors: | John Liddle Paul Bamborough Michael D Barker Sebastien Campos Chun-Wa Chung Rick P C Cousins Paul Faulder Michelle L Heathcote Heather Hobbs Duncan S Holmes Chris Ioannou Cesar Ramirez-Molina Mary A Morse Ruth Osborn Jeremy J Payne John M Pritchard William L Rumsey Daniel T Tape Giorgia Vicentini Caroline Whitworth Rick A Williamson |
| Institution: | GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK. |
| 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. |
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