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TitleDiscovery 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.
Journal, issue, pagesJ. Med. Chem., Vol. 59, Page 2328-2342, Year 2016
Publish dateNov 24, 2015 (structure data deposition date)
AuthorsBoezio, A.A. / Copeland, K.W. / Rex, K. / K Albrecht, B. / Bauer, D. / Bellon, S.F. / Boezio, C. / Broome, M.A. / Choquette, D. / Coxon, A. ...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.
External linksJ. Med. Chem. / PubMed:26812066
MethodsX-ray diffraction
Resolution1.8 - 1.85 Å
Structure data

PDB-5eyc:
Crystal structure of c-Met in complex with naphthyridinone inhibitor 5
Method: X-RAY DIFFRACTION / Resolution: 1.8 Å

PDB-5eyd:
Crystal structure of c-Met in complex with AMG 337
Method: X-RAY DIFFRACTION / Resolution: 1.85 Å

Chemicals

ChemComp-5SZ:
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

ChemComp-HOH:
WATER

ChemComp-5T1:
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

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / phosphotransferase / inhibitor / cancer / TRANSFERASE-TRANSFERASE INHIBITOR complex

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