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Updated: Jul 22, 2026

Detection of Ligand-activated G Protein-coupled Receptor Internalization by Confocal Microscopy
Published on: April 9, 2017
The discovery of tetrahydrofluorenones as a new class of estrogen receptor beta-subtype selective ligands
R R Wilkening1, R W Ratcliffe, E C Tynebor
1Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. robert_wilkening@merck.com
Abstract:
Synthesis and derivatization of a series of substituted tetrahydrofluorenone analogs giving potent, ERbeta subtype selective ligands are described. Several analogs possessing ERbeta binding affinities comparable to 17beta-estradiol but with greater than 75-fold selectivity over ERalpha are reported.
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