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