The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist.
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.
Rimland
Joseph
J
Medicines Research Centre, Verona, Italy.
Dunne
Angela
A
Hunjan
Suchete S
SS
Sasse
Rosemary
R
Uings
Iain
I
Montanari
Dino
D
Caivano
Matilde
M
Shah
Poonam
P
Standing
David
D
Gray
David
D
Brown
David
D
Cairns
William
W
Trump
Ryan
R
Smith
Paul W
PW
Bertheleme
Nicolas
N
D'Alessandro
Pier
P
Gul
Sheraz
S
Vimal
Mythily
M
Smith
David N
DN
Watson
Stephen P
SP
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
D011965:Receptors, Glucocorticoid; D054852:Small Molecule Libraries