The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist

The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist

The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A PR is described. Associated structure–activity relationships and the process of optimisation of an initial HTS hit are also described. The identification of novel, potent, non-steroidal/small molec...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2010-04, Vol.20 (7), p.2340-2343
Hauptverfasser: Rimland, Joseph, Dunne, Angela, Hunjan, Suchete S., Sasse, Rosemary, Uings, Iain, Montanari, Dino, Caivano, Matilde, Shah, Poonam, Standing, David, Gray, David, Brown, David, Cairns, William, Trump, Ryan, Smith, Paul W., Bertheleme, Nicolas, D’Alessandro, Pier, Gul, Sheraz, Vimal, Mythily, Smith, David N., Watson, Stephen P.
Format: Artikel
Sprache:eng
Schlagworte:
Animals
Biological and medical sciences
Glucocorticoid receptor
Glucocorticoid receptor antagonist
GR antagonist
Hormones. Endocrine system
Medical sciences
Pharmacology. Drug treatments
Rats
Receptors, Glucocorticoid - antagonists & inhibitors
Receptors, Glucocorticoid - metabolism
Small Molecule Libraries - chemistry
Small Molecule Libraries - metabolism
Small Molecule Libraries - pharmacology
Structure-Activity Relationship
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Zusammenfassung:The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A PR is described. Associated structure–activity relationships and the process of optimisation of an initial HTS hit are also described. The identification of novel, potent, non-steroidal/small molecule functional GR antagonist GSK1564023A selective over PR is described. Associated structure–activity relationships and the process of optimisation of an initial HTS hit are also described.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.01.133