Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo.

Article Details

Citation

Yang C, Xu G, Li J, Wu X, Liu B, Yan X, Wang M, Xie Y

Benzothiophenes containing a piperazine side chain as selective ligands for the estrogen receptor alpha and their bioactivities in vivo.

Bioorg Med Chem Lett. 2005 Mar 1;15(5):1505-7.

PubMed ID
15713417 [ View in PubMed
]
Abstract

The synthesis of benzothiophenes containing a piperazine side chain and their binding affinities for estrogen receptors are described. These compounds bearing piperazine side chains were identified to be high-affinity ligands with high selectivity for ER alpha subtype. They were also potent agonists in bone tissue.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
RaloxifeneEstrogen receptor alphaIC 50 (nM)0.73N/AN/ADetails
RaloxifeneEstrogen receptor betaIC 50 (nM)18.9N/AN/ADetails