title: The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist.
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.
authors.affiliation: Medicines Research Centre, Verona, Italy.
authors.forename: Joseph
authors.initials: J
authors.lastname: Rimland
authors.forename: Angela
authors.initials: A
authors.lastname: Dunne
authors.forename: Suchete S
authors.initials: SS
authors.lastname: Hunjan
authors.forename: Rosemary
authors.initials: R
authors.lastname: Sasse
authors.forename: Iain
authors.initials: I
authors.lastname: Uings
authors.forename: Dino
authors.initials: D
authors.lastname: Montanari
authors.forename: Matilde
authors.initials: M
authors.lastname: Caivano
authors.forename: Poonam
authors.initials: P
authors.lastname: Shah
authors.forename: David
authors.initials: D
authors.lastname: Standing
authors.forename: David
authors.initials: D
authors.lastname: Gray
authors.forename: David
authors.initials: D
authors.lastname: Brown
authors.forename: William
authors.initials: W
authors.lastname: Cairns
authors.forename: Ryan
authors.initials: R
authors.lastname: Trump
authors.forename: Paul W
authors.initials: PW
authors.lastname: Smith
authors.forename: Nicolas
authors.initials: N
authors.lastname: Bertheleme
authors.forename: Pier
authors.initials: P
authors.lastname: D'Alessandro
authors.forename: Sheraz
authors.initials: S
authors.lastname: Gul
authors.forename: Mythily
authors.initials: M
authors.lastname: Vimal
authors.forename: David N
authors.initials: DN
authors.lastname: Smith
authors.forename: Stephen P
authors.initials: SP
authors.lastname: Watson
mesh_terms: D000818:Animals; D051381:Rats; D011965:Receptors, Glucocorticoid / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D054852:Small Molecule Libraries / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D011965:Receptors, Glucocorticoid; D054852:Small Molecule Libraries