| Literature DB >> 27983835 |
Peter Jones1,2,3, R Ian Storer1,2,3, Yogesh A Sabnis1,2,3, Florian M Wakenhut1,2,3, Gavin A Whitlock1,2,3, Katherine S England1,2,3, Takasuke Mukaiyama1,2,3, Christoph M Dehnhardt1,2,3, Jotham W Coe1,2,3, Steve W Kortum1,2,3, Jill E Chrencik1,2,3, David G Brown1,2,3, Rhys M Jones1,2,3, John R Murphy1,2,3, Thean Yeoh1,2,3, Paul Morgan1,2,3, Iain Kilty1,2,3.
Abstract
By use of a structure-based computational method for identification of structurally novel Janus kinase (JAK) inhibitors predicted to bind beyond the ATP binding site, a potent series of indazoles was identified as selective pan-JAK inhibitors with a type 1.5 binding mode. Optimization of the series for potency and increased duration of action commensurate with inhaled or topical delivery resulted in potent pan-JAK inhibitor 2 (PF-06263276), which was advanced into clinical studies.Entities:
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Year: 2017 PMID： 27983835 DOI： 10.1021/acs.jmedchem.6b01634
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446