Integration of lead optimization with crystallography for a membrane-bound ion channel target: Discovery of a new class of AMPA receptor positive allosteric modulators

Journal of Medicinal Chemistry

Volumn 54, Issue 1, 2011, Pages 78-94

  Ward, Simon E ^a   Harries, Mark ^b   Aldegheri, Laura ^c   Austin, Nigel E ^b   Ballantine, Stuart ^b   Ballini, Elisa ^c   Bradley, Daniel M ^b   Bax, Benjamin D ^b   Clarke, Brian P ^b   Harris, Andrew J ^b   Harrison, Stephen A ^b   Melarange, Rosemary A ^b   Mookherjee, Claudette ^b   Mosley, Julie ^b   Dal Negro, Gianni ^c   Oliosi, Beatrice ^c   Smith, Kathrine J ^b   Thewlis, Kevin M ^b   Woollard, Patrick M ^b   Yusaf, Shahnaz P ^b  

^a UNIVERSITY OF SUSSEX   (United Kingdom)

^b GLAXOSMITHKLINE   (United Kingdom)

^c GSK   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

1 [4 (1 PYRROLIDINYLCARBONYL)PHENYL] 3 (TRIFLUOROMETHYL) 4,5,6,7 TETRAHYDRO 1H INDAZOLE; AMPA RECEPTOR; AMPA RECEPTOR AGONIST; ION CHANNEL; UNCLASSIFIED DRUG;

ALLOSTERISM; ANIMAL CELL; ANIMAL TISSUE; ARTICLE; BINDING SITE; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG EFFICACY; DRUG TOLERABILITY; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; LIGAND BINDING; MALE; NONHUMAN; RAT; REACTION OPTIMIZATION; X RAY CRYSTALLOGRAPHY;

ALLOSTERIC REGULATION; ANIMALS; CALCIUM; CRYSTALLOGRAPHY, X-RAY; DOGS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; INDAZOLES; LIGANDS; MACACA FASCICULARIS; MALE; MICROSOMES, LIVER; MODELS, MOLECULAR; MOLECULAR CONFORMATION; PATCH-CLAMP TECHNIQUES; PROTEIN MULTIMERIZATION; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, AMPA; RECOMBINANT PROTEINS; SOLUBILITY; STRUCTURE-ACTIVITY RELATIONSHIP; SWINE; SWINE, MINIATURE;

EID: 78651076694     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100679e     Document Type: Article

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