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]
- 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
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) >1 N/A N/A Details