Structure guided design of 5-arylindazole glucocorticoid receptor agonists and antagonists

Journal of Medicinal Chemistry

Volumn 53, Issue 11, 2010, Pages 4531-4544

  Yates, Christopher M ^a   Brown, Peter J ^a   Stewart, Eugene L ^a   Patten, Christopher ^b   Austin, Robert J H ^b   Holt, Jason A ^a   Maglich, Jodi M ^a   Angell, Davina C ^b   Sasse, Rosemary Z ^a   Taylor, Simon J ^b   Uings, Iain J ^b   Trump, Ryan P ^a  

^a GLAXOSMITHKLINE   (United States)

^b GLAXOSMITHKLINE   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

GLUCOCORTICOID RECEPTOR; GLUCOCORTICOID RECEPTOR ANTAGONIST; GLUTAMATE AMMONIA LIGASE; GSK 9027; HORMONE RECEPTOR STIMULATING AGENT; IMMUNOGLOBULIN ENHANCER BINDING PROTEIN; INDAZOLE DERIVATIVE; N [4 [1 (4 FLUOROPHENYL) 1H INDAZOL 5 YL] 3 (TRIFLUOROMETHYL)PHENYL] 1 PHENYLMETHANESULFONAMIDE; POLYCYCLIC AROMATIC HYDROCARBON DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DISSOCIATION; DRUG RECEPTOR BINDING; DRUG STRUCTURE; FLUORESCENCE POLARIZATION; HUMAN; HUMAN TISSUE; LIGAND BINDING; MALE; NONHUMAN; POLYMERASE CHAIN REACTION; PROTEIN EXPRESSION; QUANTITATIVE ANALYSIS; RAT; TRANSACTIVATION;

ANIMALS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; FIBROBLASTS; HUMANS; INDAZOLES; MALE; MICE; MODELS, MOLECULAR; NF-KAPPA B; PROTEIN CONFORMATION; RATS; RECEPTORS, GLUCOCORTICOID; SUBSTRATE SPECIFICITY;

EID: 77953201616     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm100447c     Document Type: Article

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