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Updated: Aug 25, 2026

A Chemical Screening Procedure for Glucocorticoid Signaling with a Zebrafish Larva Luciferase Reporter System
Published on: September 10, 2013
Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators
Steven W Elmore1, John K Pratt, Michael J Coghlan
1Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064-3500, USA. steve.elmore@abbott.com
Abstract:
The SAR at C-5 of the 10-methoxy-2,2,4-trimethylbenzopyrano[3,4-f]quinoline core leading to identification of (-) anti 1-methylcyclohexen-3-yl as the optimum substituent that imparts minimal GR mediated in vitro transcriptional activation while maintaining full transcriptional repression is described. The in vitro profile of these candidates in human cell assays relevant to the therapeutic window of glucocorticoid modulators is outlined.
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