Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.

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Elmore SW, Pratt JK, Coghlan MJ, Mao Y, Green BE, Anderson DD, Stashko MA, Lin CW, Falls D, Nakane M, Miller L, Tyree CM, Miner JN, Lane B

Differentiation of in vitro transcriptional repression and activation profiles of selective glucocorticoid modulators.

Bioorg Med Chem Lett. 2004 Apr 5;14(7):1721-7.

PubMed ID

15026058 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Prednisolone	Glucocorticoid receptor	IC 50 (nM)	2.1	N/A	N/A	Details
Prednisolone	Glucocorticoid receptor	IC 50 (nM)	8	N/A	N/A	Details