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The identification a novel,selective, non-steroidal,functional glucocorticoid receptor antagonist |
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| Authors: | 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 |
| Affiliation: | 1. GlaxoSmithKline, Neurosciences Centre of Excellence for Drug Discover, New Frontiers Science Park, Harlow, UK;2. Molecular Discovery Research, New Frontiers Science Park, Harlow, UK;3. Medicines Research Centre, Verona, Italy;4. Research Triangle Park, NC, USA;5. Immuno Inflammation Centre of Excellence for Drug Discovery, Medicines Research Centre Stevenage, UK |
| Abstract: | 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. |
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