Q4 · MEDICINE
Article
Author: Brown, Angus R. ; Kultgen, Steven G. ; Craighead, Mark ; Watson, Lynn ; Pick, Jack ; McIntyre, Theresa ; Cameron, Helen ; Kingsbury, Celia ; Sherborne, Brad ; Grove, Simon J. A. ; Firth, Alistair ; Hamilton, Niall M. ; Ho, Koc-Kan ; Hillier, Alison ; Elmore, Moira A. ; Ohlmeyer, Michael ; Nimz, Olaf ; MacDonald, Susan ; Weston, Mark ; Mistry, Ashvin ; Rankovic, Zoran ; Lusher, Scott J. ; Cowley, Angela ; Morphy, J. Richard ; McIntosh, Lorraine ; Littlewood, Peter T. A. ; Spinks, Gayle ; Goodwin, Richard ; Speake, Michael ; Bosies, Michael ; Goutcher, Susan ; Smith, Alasdair ; Hampson, Hannah ; Grassie, Morag ; Grant, Emma ; Thomson, Fiona ; Kiczun, Michael ; Clark, John
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.