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Discovery and optimization of novel, non-steroidal glucocorticoid receptor modulators |
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| Authors: | Ray Nicholas C Clark Robin D Clark David E Williams Karen Hickin H G Crackett Peter H Dyke Hazel J Lockey Peter M Wong Melanie Devos René White Anne Belanoff Joseph K |
| Affiliation: | Argenta Discovery Ltd, 8/9 Spire Green Centre, Flex Meadow, Harlow, Essex, UK. nick.ray@argentadiscovery.com |
| Abstract: | A virtual screening approach comprising a 3-D similarity search based on known GR modulators was used to identify a novel series of non-steroidal glucocorticoid receptor (GR) antagonists. Optimization of the initial hit to provide potent compounds which exhibit good selectivity against other steroidal nuclear hormone receptors is described. |
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