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TitleDiscovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer.
Journal, issue, pagesJ. Med. Chem., Vol. 63, Page 512-528, Year 2020
Publish dateJul 22, 2019 (structure data deposition date)
AuthorsEl-Ahmad, Y. / Tabart, M. / Halley, F. / Certal, V. / Thompson, F. / Filoche-Romme, B. / Gruss-Leleu, F. / Muller, C. / Brollo, M. / Fabien, L. ...El-Ahmad, Y. / Tabart, M. / Halley, F. / Certal, V. / Thompson, F. / Filoche-Romme, B. / Gruss-Leleu, F. / Muller, C. / Brollo, M. / Fabien, L. / Loyau, V. / Bertin, L. / Richepin, P. / Pilorge, F. / Desmazeau, P. / Girardet, C. / Beccari, S. / Louboutin, A. / Lebourg, G. / Le-Roux, J. / Terrier, C. / Vallee, F. / Steier, V. / Mathieu, M. / Rak, A. / Abecassis, P.Y. / Vicat, P. / Benard, T. / Bouaboula, M. / Sun, F. / Shomali, M. / Hebert, A. / Levit, M. / Cheng, H. / Courjaud, A. / Ginesty, C. / Perrault, C. / Garcia-Echeverria, C. / McCort, G. / Schio, L.
External linksJ. Med. Chem. / PubMed:31721572
MethodsX-ray diffraction
Resolution1.48 Å
Structure data

PDB-6sbo:
Estrogen receptor mutant L536S
Method: X-RAY DIFFRACTION / Resolution: 1.48 Å

Chemicals

ChemComp-L5B:
6-(2,4-dichlorophenyl)-5-[4-[(3~{S})-1-(3-fluoranylpropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7~{H}-benzo[7]annulene-2-carboxylic acid

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION / receptor

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