Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.

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Roach SL, Higuchi RI, Adams ME, Liu Y, Karanewsky DS, Marschke KB, Mais DE, Miner JN, Zhi L

Discovery of nonsteroidal glucocorticoid receptor ligands based on 6-indole-1,2,3,4-tetrahydroquinolines.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3504-8. doi: 10.1016/j.bmcl.2008.05.029. Epub 2008 May 11.

PubMed ID
18513967 [ View in PubMed
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Abstract

A series of nonsteroidal glucocorticoid receptor (GR) ligands based on a 6-indole-1,2,3,4-tetrahydroquinoline scaffold are reported. Structure-activity relationship (SAR) of the pendent indole group identified compound 20 exhibiting good GR binding affinity (K(i)=1.5nM) and 100- to 1000-fold selectivity over MR, PR, and AR while showing activity in an E-selectin repression assay.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
PrednisoloneGlucocorticoid receptorEC 50 (nM)5.3N/AN/ADetails
PrednisoloneGlucocorticoid receptorKi (nM)5.3N/AN/ADetails
PrednisoloneGlucocorticoid receptorIC 50 (nM)4.1N/AN/ADetails
PrednisoloneGlucocorticoid receptorIC 50 (nM)>1N/AN/ADetails