Androstenediol analogs as ER-beta-selective SERMs.

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Blizzard TA, Gude C, Morgan JD 2nd, Chan W, Birzin ET, Mojena M, Tudela C, Chen F, Knecht K, Su Q, Kraker B, Mosley RT, Holmes MA, Sharma N, Fitzgerald PM, Rohrer SP, Hammond ML

Androstenediol analogs as ER-beta-selective SERMs.

Bioorg Med Chem Lett. 2006 Feb 15;16(4):834-8. Epub 2005 Nov 23.

PubMed ID
16309907 [ View in PubMed
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Abstract

A series of 19-substituted androstenediol derivatives was prepared. Some of the novel analogs were surprisingly potent and selective ligands for ER-beta.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
EstradiolEstrogen receptor alphaIC 50 (nM)1.4N/AN/ADetails
EstradiolEstrogen receptor alphaEC 50 (nM)0.75N/AN/ADetails
EstradiolEstrogen receptor betaIC 50 (nM)1.2N/AN/ADetails
EstradiolEstrogen receptor betaEC 50 (nM)2.1N/AN/ADetails
TestosteroneAndrogen receptorIC 50 (nM)2.7N/AN/ADetails
TestosteroneEstrogen receptor alphaIC 50 (nM)>10000N/AN/ADetails