Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity.

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Chen HY, Dykstra KD, Birzin ET, Frisch K, Chan W, Yang YT, Mosley RT, DiNinno F, Rohrer SP, Schaeffer JM, Hammond ML

Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity.

Bioorg Med Chem Lett. 2004 Mar 22;14(6):1417-21.

PubMed ID
15006374 [ View in PubMed
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Abstract

A class of flavanoids exhibiting a high degree of selectivity for ERalpha over ERbeta has been discovered. The most active analogue 6 was found to be 66-fold ERalpha-selective and demonstrated uterine estradiol antagonism.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
EstradiolEstrogen receptor alphaIC 50 (nM)1.3N/AN/ADetails
EstradiolEstrogen receptor betaIC 50 (nM)1.1N/AN/ADetails
GenisteinEstrogen receptor alphaIC 50 (nM)92N/AN/ADetails
GenisteinEstrogen receptor betaIC 50 (nM)4N/AN/ADetails
RaloxifeneEstrogen receptor alphaIC 50 (nM)1.8N/AN/ADetails
RaloxifeneEstrogen receptor betaIC 50 (nM)12N/AN/ADetails