Diazinones as P2 replacements for pyrazole-based cathepsin S inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 14, 2010, Pages 4060-4064

  Ameriks, Michael K ^a   Bembenek, Scott D ^a   Burdett, Matthew T ^b   Choong, Ingrid C ^b   Edwards, James P ^a   Gebauer, Damara ^a   Gu, Yin ^a   Karlsson, Lars ^a   Purkey, Hans E ^b   Staker, Bart L ^c   Sun, Siquan ^a   Thurmond, Robin L ^a   Zhu, Jian ^a  

^a JOHNSON AND JOHNSON PHARMACEUTICAL RESEARCH AND DEVELOPMENT   (United States)

^b Sunesis Pharmaceuticals Inc   (United States)

^c DeCODE Chemistry & Biostructures   (United States)

Author keywords

Cathepsin; Fragment based screening; Protease; Tethering; X ray crystallography

Indexed keywords

CATHEPSIN S INHIBITOR; DIAZINONE DERIVATIVE; PYRAZOLE; PYRIDAZINONE DERIVATIVE; UNCLASSIFIED DRUG;

ARTICLE; CRYSTAL STRUCTURE; DRUG STRUCTURE; ENZYME ACTIVITY; HIGH THROUGHPUT SCREENING; ISOMER;

CATHEPSINS; CRYSTALLOGRAPHY, X-RAY; MODELS, MOLECULAR; PROTEASE INHIBITORS; PYRAZOLES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77953872634     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.05.086     Document Type: Article

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