Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists.

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Hudson AR, Higuchi RI, Roach SL, Adams ME, Vassar A, Syka PM, Mais DE, Miner JN, Marschke KB, Zhi L

Discovery of orally available tetrahydroquinoline-based glucocorticoid receptor agonists.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1697-700. doi: 10.1016/j.bmcl.2011.01.093. Epub 2011 Jan 26.

PubMed ID

21316964 [ View in PubMed

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Abstract

A series of tetrahydroquinoline derivatives were synthesized and profiled for their ability to act as glucocorticoid receptor selective modulators. Structure-activity relationships of the tetrahydroquinoline B-ring lead to the discovery of orally available GR-selective agonists with high in vivo activity.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Prednisolone	Glucocorticoid receptor	EC 50 (nM)	5.3	N/A	N/A	Details
Prednisolone	Glucocorticoid receptor	Ki (nM)	5.3	N/A	N/A	Details
Prednisolone	Glucocorticoid receptor	IC 50 (nM)	4.1	N/A	N/A	Details
Prednisolone	Glucocorticoid receptor	IC 50 (nM)	23	N/A	N/A	Details