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-Structure paper
Title | Discovery of a C-8 hydroxychromene as a potent degrader of estrogen receptor alpha with improved rat oral exposure over GDC-0927. |
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Journal, issue, pages | Bioorg. Med. Chem. Lett., Vol. 29, Page 2090-2093, Year 2019 |
Publish date | Jun 20, 2019 (structure data deposition date) |
Authors | Labadie, S.S. / Li, J. / Blake, R.A. / Chang, J.H. / Goodacre, S. / Hartman, S.J. / Liang, W. / Kiefer, J.R. / Kleinheinz, T. / Lai, T. ...Labadie, S.S. / Li, J. / Blake, R.A. / Chang, J.H. / Goodacre, S. / Hartman, S.J. / Liang, W. / Kiefer, J.R. / Kleinheinz, T. / Lai, T. / Liao, J. / Ortwine, D.F. / Mody, V. / Ray, N.C. / Roussel, F. / Vinogradova, M. / Yeap, S.K. / Zhang, B. / Zheng, X. / Zbieg, J.R. / Liang, J. / Wang, X. |
External links | Bioorg. Med. Chem. Lett. / PubMed:31311734 |
Methods | X-ray diffraction |
Resolution | 2.203 - 2.84 Å |
Structure data | PDB-6pet: PDB-6pfm: |
Chemicals | ChemComp-G9J: ChemComp-ODY: ChemComp-CL: ChemComp-DMS: ChemComp-HOH: ChemComp-OGJ: |
Source |
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Keywords | NUCLEAR PROTEIN / hormone receptor / ligand / breast cancer / drug / antagonist |