Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.

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Blizzard TA, Morgan JD 2nd, Chan W, Birzin ET, Pai LY, Hayes EC, DaSilva CA, Mosley RT, Yang YT, Rohrer SP, Dininno F, Hammond ML

Estrogen receptor ligands. Part 14: application of novel antagonist side chains to existing platforms.

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5124-8. Epub 2005 Oct 3.

PubMed ID

16203138 [ View in PubMed

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Abstract

Two novel side chains which had previously been found to enhance antagonist activity in the dihydrobenzoxathiin SERM series were applied to three existing platforms. The novel side chains did not improve the antagonist activity of the existing platforms.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Compound 18	Estrogen receptor alpha	IC 50 (nM)	1.3	N/A	N/A	Details
Raloxifene	Estrogen receptor alpha	IC 50 (nM)	1.8	N/A	N/A	Details
Raloxifene	Estrogen receptor beta	IC 50 (nM)	12	N/A	N/A	Details