Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.
Article Details
- CitationCopy to clipboard
Chesworth R, Wessel MD, Heyden L, Mangano FM, Zawistoski M, Gegnas L, Galluzzo D, Lefker B, Cameron KO, Tickner J, Lu B, Castleberry TA, Petersen DN, Brault A, Perry P, Ng O, Owen TA, Pan L, Ke HZ, Brown TA, Thompson DD, DaSilva-Jardine P
Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.
Bioorg Med Chem Lett. 2005 Dec 15;15(24):5562-6. Epub 2005 Oct 10.
- PubMed ID
- 16219463 [ View in PubMed]
- Abstract
A series of ligands with varying heterocyclic cores and substituents that display a range of selectivity's (up to >100x) for ER-beta over ER-alpha are reported.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Estradiol Estrogen receptor alpha IC 50 (nM) 0.75 N/A N/A Details Estradiol Estrogen receptor alpha EC 50 (nM) 0.01 N/A N/A Details Estradiol Estrogen receptor beta IC 50 (nM) 1.18 N/A N/A Details Genistein Estrogen receptor alpha IC 50 (nM) 29.4 N/A N/A Details Genistein Estrogen receptor beta IC 50 (nM) 1.3 N/A N/A Details