| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1363332 | Bioorganic & Medicinal Chemistry Letters | 2010 | 4 Pages |
Abstract
Morphing structural features of HTS-derived chemotypes led to the discovery of novel 2-cyano-pyrimidine inhibitors of cathepsin K with good pharmacokinetic profiles, for example, compound 20 showed high catK potency (IC50 = 4 nM), >580-fold selectivity over catL and catB, and oral bioavailability in the rat of 52%.
Graphical abstractMorphing structural features of HTS-derived chemotypes led to the discovery of novel 2-cyano-pyrimidine inhibitors of cathepsin K with improved pharmacokinetic profile.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Zoran Rankovic, Jiaqiang Cai, Jennifer Kerr, Xavier Fradera, John Robinson, Ashvin Mistry, Emma Hamilton, George McGarry, Fiona Andrews, Wilson Caulfield, Iain Cumming, Maureen Dempster, John Waller, Paul Scullion, Iain Martin, Ann Mitchell, Clive Long,