Estrogen receptor beta ligands: design and synthesis of new 2-phenyl-isoindole-1,3-diones.

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Ullrich JW, Unwalla RJ, Singhaus RR Jr, Harris HA, Mewshaw RE

Estrogen receptor beta ligands: design and synthesis of new 2-phenyl-isoindole-1,3-diones.

Bioorg Med Chem Lett. 2007 Jan 1;17(1):118-22. Epub 2006 Oct 1.

PubMed ID
17049855 [ View in PubMed
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Abstract

The design, synthesis, and biological evaluation of the 2-phenyl-isoindole-1,3-diones will be discussed. Detailed modeling studies with X-ray support were used to understand the ligand binding orientation and observed selectivity.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
EstradiolEstrogen receptor alphaIC 50 (nM)3.6N/AN/ADetails
EstradiolEstrogen receptor betaIC 50 (nM)3.2N/AN/ADetails
GenisteinEstrogen receptor alphaIC 50 (nM)9.7N/AN/ADetails
GenisteinEstrogen receptor betaIC 50 (nM)395N/AN/ADetails