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TitleDiscovery and Optimization of Triazolopyridazines as Potent and Selective Inhibitors of the c-Met Kinase.
Journal, issue, pagesJ. Med. Chem., Vol. 51, Page 2879-2882, Year 2008
Publish dateFeb 26, 2008 (structure data deposition date)
AuthorsAlbrecht, B.K. / Harmange, J.C. / Bauer, D. / Berry, L. / Bode, C. / Boezio, A.A. / Chen, A. / Choquette, D. / Dussault, I. / Fridrich, C. ...Albrecht, B.K. / Harmange, J.C. / Bauer, D. / Berry, L. / Bode, C. / Boezio, A.A. / Chen, A. / Choquette, D. / Dussault, I. / Fridrich, C. / Hirai, S. / Hoffman, D. / Larrow, J.F. / Kaplan-Lefko, P. / Lin, J. / Lohman, J. / Long, A.M. / Moriguchi, J. / O'Connor, A. / Potashman, M.H. / Reese, M. / Rex, K. / Siegmund, A. / Shah, K. / Shimanovich, R. / Springer, S.K. / Teffera, Y. / Yang, Y. / Zhang, Y. / Bellon, S.F.
External linksJ. Med. Chem. / PubMed:18426196
MethodsX-ray diffraction
Resolution1.9 - 2 Å
Structure data

PDB-3ccn:
X-ray structure of c-Met with triazolopyridazine inhibitor.
Method: X-RAY DIFFRACTION / Resolution: 1.9 Å

PDB-3cd8:
X-ray Structure of c-Met with triazolopyridazine Inhibitor.
Method: X-RAY DIFFRACTION / Resolution: 2 Å

Chemicals

ChemComp-LKG:
4-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methyl]phenol

ChemComp-HOH:
WATER

ChemComp-L5G:
7-methoxy-4-[(6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / c-Met Kinase Triazolopyridazine / ATP-binding / Glycoprotein / Membrane / Nucleotide-binding / Phosphoprotein / Proto-oncogene / Receptor / Transmembrane / Tyrosine-protein kinase / c-Met / Kinase / Triazolopyridazine

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