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The identification a novel, selective, non-steroidal, functional glucocorticoid receptor antagonist.

Authors :
Rimland J
Dunne A
Hunjan SS
Sasse R
Uings I
Montanari D
Caivano M
Shah P
Standing D
Gray D
Brown D
Cairns W
Trump R
Smith PW
Bertheleme N
D'Alessandro P
Gul S
Vimal M
Smith DN
Watson SP
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 Apr 01; Vol. 20 (7), pp. 2340-3. Date of Electronic Publication: 2010 Feb 04.
Publication Year :
2010

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.<br /> (2010 Elsevier Ltd. All rights reserved.)

Details

Language :
English
ISSN :
1464-3405
Volume :
20
Issue :
7
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
20202837
Full Text :
https://doi.org/10.1016/j.bmcl.2010.01.133