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Updated: Aug 7, 2026

Detecting the Ligand-binding Domain Dimerization Activity of Estrogen Receptor Alpha Using the Mammalian Two-Hybrid Assay
Published on: December 19, 2018
Triazolo-tetrahydrofluorenones as selective estrogen receptor beta agonists
Dann L Parker1, Dongfang Meng, Ronald W Ratcliffe
1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, NJ 07065, USA. dann_parker@merck.com
Abstract:
Several tetrahydrofluorenones with a triazole fused across C7-C8 showed high levels of ERbeta-selectivity and were found to be potent ERbeta-agonists. As a class they demonstrate improved oral bioavailability in the rat over a parent class of 7-hydroxy-tetrahydrofluorenones. The most selective agonist displayed 5.7 nM affinity and 333-fold selectivity for ERbeta.
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