Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.

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Richards SJ, von Geldern TW, Jacobson P, Wilcox D, Nguyen P, Ohman L, Osterlund M, Gelius B, Grynfarb M, Goos-Nilsson A, Wang J, Fung S, Kalmanovich M

Synthesis and activity of novel bile-acid conjugated glucocorticoid receptor antagonists.

Bioorg Med Chem Lett. 2006 Dec 1;16(23):6086-90. Epub 2006 Sep 20.

PubMed ID

16987661 [ View in PubMed

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Abstract

A series of potent steroidal glucocorticoid receptor antagonists has been discovered. After conjugation to cholic acid, the compounds retained an affinity for GR in vitro and had modest in vivo efficacy.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Mifepristone	Glucocorticoid receptor	IC 50 (nM)	1.1	N/A	N/A	Details
Mifepristone	Glucocorticoid receptor	IC 50 (nM)	5	N/A	N/A	Details