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

Joseph Rimland,Angela Dunne,Suchete S Hunjan,Rosemary Sasse,Iain Uings,Dino Montanari,Matilde Caivano,Poonam Shah,David Standing,David Gray,David Brown,William Cairns,Ryan Trump,Paul W Smith,Nicolas Bertheleme,Pier D'Alessandro,Sheraz Gul,Mythily Vimal,David N Smith,Stephen P Watson

Bioorganic & Medicinal Chemistry Letters（2010）

Cited 11|Views24
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Abstract
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.
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Key words
GR antagonist,Glucocorticoid receptor,Glucocorticoid receptor antagonist
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