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Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist

By Angus R. Brown, Michael Bosies, Helen Cameron, John Clark, Angela Cowley, Mark Craighead, Moira A. Elmore, Alistair Firth, Richard Goodwin, Susan Goutcher, Emma Grant, Morag Grassie, Simon J.A. Grove, Niall M. Hamilton, Hannah Hampson, Alison Hillier, Koc-Kan Ho, Michael Kiczun, Celia Kingsbury, Steven G. Kultgen, Peter T.A. Littlewood, Scott J. Lusher, Susan MacDonald, Lorraine McIntosh, Theresa McIntyre, Ashvin Mistry, J. Richard Morphy, Olaf Nimz, Michael Ohlmeyer, Jack Pick, Zoran Rankovic, Brad Sherborne, Alasdair Smith, Michael Speake, Gayle Spinks, Fiona Thomson, Lynn Watson and Mark Weston


High-throughput screening of 3.87 million compounds delivered a novel series of non-steroidal GR antagonists. Subsequent rounds of optimisation allowed progression from a non-selective ligand with a poor ADMET profile to an orally bioavailable, selective, stable, glucocorticoid receptor antagonist

Publisher: Elsevier
Year: 2011
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Provided by: Enlighten
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