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TitleDesign, synthesis, and biological evaluation of potent c-Met inhibitors.
Journal, issue, pagesJ. Med. Chem., Vol. 51, Page 5766-5779, Year 2008
Publish dateSep 9, 2008 (structure data deposition date)
AuthorsD'Angelo, N.D. / Bellon, S.F. / Booker, S.K. / Cheng, Y. / Coxon, A. / Dominguez, C. / Fellows, I. / Hoffman, D. / Hungate, R. / Kaplan-Lefko, P. ...D'Angelo, N.D. / Bellon, S.F. / Booker, S.K. / Cheng, Y. / Coxon, A. / Dominguez, C. / Fellows, I. / Hoffman, D. / Hungate, R. / Kaplan-Lefko, P. / Lee, M.R. / Li, C. / Liu, L. / Rainbeau, E. / Reider, P.J. / Rex, K. / Siegmund, A. / Sun, Y. / Tasker, A.S. / Xi, N. / Xu, S. / Yang, Y. / Zhang, Y. / Burgess, T.L. / Dussault, I. / Kim, T.S.
External linksJ. Med. Chem. / PubMed:18763753
MethodsX-ray diffraction
Resolution2.2 - 2.6 Å
Structure data

PDB-3efj:
Structure of c-Met with pyrimidone inhibitor 7
Method: X-RAY DIFFRACTION / Resolution: 2.6 Å

PDB-3efk:
Structure of c-Met with pyrimidone inhibitor 50
Method: X-RAY DIFFRACTION / Resolution: 2.2 Å

Chemicals

ChemComp-MT3:
2-benzyl-5-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-3-methylpyrimidin-4(3H)-one

ChemComp-HOH:
WATER

ChemComp-MT4:
5-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]-3-fluorophenyl}-2-[(4-fluorophenyl)amino]-3-methylpyrimidin-4(3H)-one

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / c-Met / Alternative splicing / ATP-binding / Chromosomal rearrangement / Disease mutation / Glycoprotein / Kinase / Membrane / Nucleotide-binding / Phosphoprotein / Polymorphism / Proto-oncogene / Receptor / Transmembrane / Tyrosine-protein kinase / Kinase inhibitor pyrimidone

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