Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: Improving selectivity over hERG

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 21, 2010, Pages 6237-6241

  Rankovic, Zoran ^a   Cai, Jiaqiang ^a   Kerr, Jennifer ^a   Fradera, Xavier ^a   Robinson, John ^a   Mistry, Ashvin ^a   Finlay, William ^a   McGarry, George ^a   Andrews, Fiona ^a   Caulfield, Wilson ^a   Cumming, Iain ^a   Dempster, Maureen ^a   Waller, John ^a   Arbuckle, Wullie ^a   Anderson, Mark ^a   Martin, Iain ^a   Mitchell, Ann ^a   Long, Clive ^a   Baugh, Mark ^a   Westwood, Paul ^a   Kinghorn, Emma ^a   Jones, Phil ^a   Uitdehaag, Joost C M ^a   Van Zeeland, Mario ^a   Potin, Dominique ^b   Saniere, Laurent ^b   Fouquet, Andre ^b   Chevallier, Franois ^b   Deronzier, Hortense ^b   Dorleans, Cecile ^b   Nicolai, Eric ^b   more..

^a MERCK RESEARCH LABORATORIES   (United States)

^b CEREP   (France)

Author keywords

Cathepsin K; Cysteine protease; Osteoporosis

Indexed keywords

CATHEPSIN K; CATHEPSIN K INHIBITOR; POTASSIUM CHANNEL HERG; PYRIMIDINE DERIVATIVE;

ARTICLE; CELL STRAIN HEK293; DRUG EFFICACY; DRUG STRUCTURE; DRUG SYNTHESIS; IN VITRO STUDY; IN VIVO STUDY; OSTEOLYSIS; OSTEOPOROSIS; STRUCTURE ACTIVITY RELATION;

CATHEPSIN K; DRUG DESIGN; DRUG DISCOVERY; ETHER-A-GO-GO POTASSIUM CHANNELS; INDICATORS AND REAGENTS; MODELS, MOLECULAR; NITRILES; POTASSIUM CHANNEL BLOCKERS; PYRIMIDINES; ROC CURVE; STRUCTURE-ACTIVITY RELATIONSHIP; TORSADES DE POINTES;

EID: 77957879523     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.08.101     Document Type: Article

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