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| Title | Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a Potent and Selective Inhibitor of Histone Methyltransferase EZH2, Suitable for Phase I Clinical Trials for B-Cell Lymphomas. |
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| Journal, issue, pages | J. Med. Chem., Vol. 59, Page 9928-9941, Year 2016 |
| Publish date | Aug 22, 2016 (structure data deposition date) |
Authors | Vaswani, R.G. / Gehling, V.S. / Dakin, L.A. / Cook, A.S. / Nasveschuk, C.G. / Duplessis, M. / Iyer, P. / Balasubramanian, S. / Zhao, F. / Good, A.C. ...Vaswani, R.G. / Gehling, V.S. / Dakin, L.A. / Cook, A.S. / Nasveschuk, C.G. / Duplessis, M. / Iyer, P. / Balasubramanian, S. / Zhao, F. / Good, A.C. / Campbell, R. / Lee, C. / Cantone, N. / Cummings, R.T. / Normant, E. / Bellon, S.F. / Albrecht, B.K. / Harmange, J.C. / Trojer, P. / Audia, J.E. / Zhang, Y. / Justin, N. / Chen, S. / Wilson, J.R. / Gamblin, S.J. |
External links | J. Med. Chem. / PubMed:27739677 |
| Methods | X-ray diffraction |
| Resolution | 3.47 Å |
| Structure data | ![]() PDB-5ls6: |
| Chemicals | ![]() ChemComp-ZN: ![]() ChemComp-74D: |
| Source |
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Keywords | Transferase/Inhibitor / Human PRC2 / Inhibitor / H3K27 / Transferase-Inhibitor complex |
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homo sapiens (human)
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