1257301-91-9Relevant academic research and scientific papers
Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: Improving selectivity over hERG
Rankovic, Zoran,Cai, Jiaqiang,Kerr, Jennifer,Fradera, Xavier,Robinson, John,Mistry, Ashvin,Finlay, William,McGarry, George,Andrews, Fiona,Caulfield, Wilson,Cumming, Iain,Dempster, Maureen,Waller, John,Arbuckle, Wullie,Anderson, Mark,Martin, Iain,Mitchell, Ann,Long, Clive,Baugh, Mark,Westwood, Paul,Kinghorn, Emma,Jones, Phil,Uitdehaag, Joost C.M.,Van Zeeland, Mario,Potin, Dominique,Saniere, Laurent,Fouquet, Andre,Chevallier, Franois,Deronzier, Hortense,Dorleans, Cecile,Nicolai, Eric
, p. 6237 - 6241 (2010)
Several structure-guided optimisation strategies were explored in order to improve the hERG selectivity profile of cathepsin K inhibitor 1, whilst maintaining its otherwise excellent in vitro and in vivo profile. Ultimately, attenuation of c log P and pK
