Novel and selective spiroindoline-based inhibitors of sky kinase

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 1, 2012, Pages 190-193

  Powell, Noel A ^a,b   Kohrt, Jeffrey T ^a   Filipski, Kevin J ^a   Kaufman, Michael ^a   Sheehan, Derek ^a   Edmunds, Jeremy E ^a   Delaney, Amy ^a   Wang, Yuli ^a   Bourbonais, Francis ^a   Lee, Doh Yeel ^a   Schwende, Frank ^a   Sun, Fang ^a   McConnell, Pat ^a   Catana, Cornel ^a   Chen, Huifen ^a   Ohren, Jeff ^a   Perrin, Lisa A ^a  

^a PFIZER INC   (United States)

^b Proteostasis Therapeutics   (United States)

Author keywords

Crystal structure; Kinase inhibitor; Platelet aggregation

Indexed keywords

ADENOSINE TRIPHOSPHATE; CYTOCHROME P450 2D6; GROWTH ARREST SPECIFIC PROTEIN 6; PHOSPHOTRANSFERASE INHIBITOR; SPIROINDOLINE 2 CARBOXYINDOLE; UNCLASSIFIED DRUG;

ARTICLE; BINDING SITE; CHEMICAL STRUCTURE; CRYSTAL STRUCTURE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG METABOLISM; DRUG POTENCY; DRUG SELECTIVITY; ENANTIOMER; ENZYME ACTIVITY; ENZYME INHIBITION; IC 50; IN VITRO STUDY; INTESTINE; NONHUMAN; PROTEIN BINDING; RAT; THROMBOCYTE AGGREGATION;

ABSORPTION; ADENOSINE TRIPHOSPHATE; ADMINISTRATION, ORAL; ANIMALS; BINDING SITES; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; HUMANS; INHIBITORY CONCENTRATION 50; INTESTINES; MODELS, CHEMICAL; PLATELET AGGREGATION; RATS; RECEPTOR PROTEIN-TYROSINE KINASES;

RATTUS;

EID: 84655164835     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.11.036     Document Type: Article

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11. Coordinates for the Sky/11 complex (pdb ID code: 3QUP) have been deposited at www.rcsb.org.
12. 50 data for individual kinases in the broad screening panel can be found in the Supplementary data.