5EYC
Crystal structure of c-Met in complex with naphthyridinone inhibitor 5
Summary for 5EYC
Entry DOI | 10.2210/pdb5eyc/pdb |
Related | 5EYD |
Descriptor | Hepatocyte growth factor receptor, 6-[(1~{R})-1-[8-fluoranyl-6-(3-methyl-1,2-oxazol-5-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl]-1,6-naphthyridin-5-one (3 entities in total) |
Functional Keywords | phosphotransferase, inhibitor, cancer, transferase-transferase inhibitor complex, transferase/transferase inhibitor |
Biological source | Homo sapiens (Human) |
Cellular location | Membrane; Single-pass type I membrane protein. Isoform 3: Secreted: P08581 |
Total number of polymer chains | 1 |
Total formula weight | 35606.09 |
Authors | Whittington, D.A.,Long, A.M. (deposition date: 2015-11-24, release date: 2016-02-10, Last modification date: 2023-09-27) |
Primary citation | Boezio, A.A.,Copeland, K.W.,Rex, K.,K Albrecht, B.,Bauer, D.,Bellon, S.F.,Boezio, C.,Broome, M.A.,Choquette, D.,Coxon, A.,Dussault, I.,Hirai, S.,Lewis, R.,Lin, M.H.,Lohman, J.,Liu, J.,Peterson, E.A.,Potashman, M.,Shimanovich, R.,Teffera, Y.,Whittington, D.A.,Vaida, K.R.,Harmange, J.C. Discovery of (R)-6-(1-(8-Fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one (AMG 337), a Potent and Selective Inhibitor of MET with High Unbound Target Coverage and Robust In Vivo Antitumor Activity. J.Med.Chem., 59:2328-2342, 2016 Cited by PubMed: 26812066DOI: 10.1021/acs.jmedchem.5b01716 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (1.8 Å) |
Structure validation
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