1268486-70-9Relevant academic research and scientific papers
Discovery and optimisation of a selective non-steroidal glucocorticoid receptor antagonist
Brown, Angus R.,Bosies, Michael,Cameron, Helen,Clark, John,Cowley, Angela,Craighead, Mark,Elmore, Moira A.,Firth, Alistair,Goodwin, Richard,Goutcher, Susan,Grant, Emma,Grassie, Morag,Grove, Simon J.A.,Hamilton, Niall M.,Hampson, Hannah,Hillier, Alison,Ho, Koc-Kan,Kiczun, Michael,Kingsbury, Celia,Kultgen, Steven G.,Littlewood, Peter T.A.,Lusher, Scott J.,MacDonald, Susan,McIntosh, Lorraine,McIntyre, Theresa,Mistry, Ashvin,Morphy, J. Richard,Nimz, Olaf,Ohlmeyer, Michael,Pick, Jack,Rankovic, Zoran,Sherborne, Brad,Smith, Alasdair,Speake, Michael,Spinks, Gayle,Thomson, Fiona,Watson, Lynn,Weston, Mark
scheme or table, p. 137 - 140 (2011/02/27)
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.
