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TitleDiscovery of 1-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]-N-(pyridin-2-ylmethyl)methanesulfonamide (MK-8033): A Specific c-Met/Ron dual kinase inhibitor with preferential affinity for the activated state of c-Met.
Journal, issue, pagesJ. Med. Chem., Vol. 56, Page 2294-2310, Year 2013
Publish dateJan 23, 2013 (structure data deposition date)
AuthorsNorthrup, A.B. / Katcher, M.H. / Altman, M.D. / Chenard, M. / Daniels, M.H. / Deshmukh, S.V. / Falcone, D. / Guerin, D.J. / Hatch, H. / Li, C. ...Northrup, A.B. / Katcher, M.H. / Altman, M.D. / Chenard, M. / Daniels, M.H. / Deshmukh, S.V. / Falcone, D. / Guerin, D.J. / Hatch, H. / Li, C. / Lu, W. / Lutterbach, B. / Allison, T.J. / Patel, S.B. / Reilly, J.F. / Reutershan, M. / Rickert, K.W. / Rosenstein, C. / Soisson, S.M. / Szewczak, A.A. / Walker, D. / Wilson, K. / Young, J.R. / Pan, B.S. / Dinsmore, C.J.
External linksJ. Med. Chem. / PubMed:23379595
MethodsX-ray diffraction
Resolution1.99 Å
Structure data

PDB-4iwd:
Structure of dually phosphorylated c-MET receptor kinase in complex with an MK-8033 analog
Method: X-RAY DIFFRACTION / Resolution: 1.99 Å

Chemicals

ChemComp-1JC:
1-{5-oxo-3-[1-(piperidin-4-yl)-1H-pyrazol-4-yl]-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl}-N-(pyridin-2-ylmethyl)methanesulfonamide

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSFERASE/TRANSFERASE INHIBITOR / Protein kinase / tyrosine kinase / TRANSFERASE-TRANSFERASE INHIBITOR complex

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