Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593061 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
SAR was used to further develop an indazole class of non-steroidal glucocorticoid receptor agonists aided by a GR LBD (ligand-binding domain)-agonist co-crystal structure described in the accompanying paper. Progress towards discovering a dissociated GR agonist guided by human in vitro assays biased the optimization of this compound series towards partial agonists that possessed excellent selectivity against other nuclear hormone receptors.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
John L. Gilmore, James E. II, Jim Wang, T.G. Murali Dhar, Cullen Cavallaro, Arthur M. Doweyko, Lorraine Mckay, Mark D. Cunningham, Sium F. Habte, Steven G. Nadler, John H. Dodd, John E. Somerville, Joel C. Barrish,