5EYD

Crystal structure of c-Met in complex with AMG 337

Summary for 5EYD

• Entry DOI: 10.2210/pdb5eyd/pdb
• Related: 5EYC
• Descriptor: Hepatocyte growth factor receptor, 6-[(1~{R})-1-[8-fluoranyl-6-(1-methylpyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl]ethyl]-3-(2-methoxyethoxy)-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: 35679.18

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; PubMed: 26812066; DOI: 10.1021/acs.jmedchem.5b01716

Experimental method

X-RAY DIFFRACTION (1.85 Å)