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TitleLessons from (S)-6-(1-(6-(1-Methyl-1H-Pyrazol-4-Yl)-[1,2, 4]Triazolo[4,3-B]Pyridazin-3-Yl)Ethyl)Quinoline (Pf-04254644), an Inhibitor of Receptor Tyrosine Kinase C-met with High Protein Kinase Selectivity But Broad Phosphodiesterase Family Inhibition Leading to Myocardial Degeneration in Rats.
Journal, issue, pagesJ. Med. Chem., Vol. 56, Page 6651-, Year 2013
Publish dateNov 13, 2012 (structure data deposition date)
AuthorsCui, J.J. / Shen, H. / Tran-Dube, M. / Nambu, M. / Mctigue, M. / Grodsky, N. / Ryan, K. / Yamazaki, S. / Aguirre, S. / Parker, M. ...Cui, J.J. / Shen, H. / Tran-Dube, M. / Nambu, M. / Mctigue, M. / Grodsky, N. / Ryan, K. / Yamazaki, S. / Aguirre, S. / Parker, M. / Li, Q. / Zou, H. / Christensen, J.
External linksJ. Med. Chem. / PubMed:23944843
MethodsX-ray diffraction
Resolution1.4 - 2.2 Å
Structure data

PDB-3zbx:
X-ray Structure of c-Met kinase in complex with inhibitor 6-((6-(4- fluorophenyl)-(1,2,4)triazolo(4,3-b)(1,2,4)triazin-3-yl)methyl) quinoline.
Method: X-RAY DIFFRACTION / Resolution: 2.2 Å

PDB-3zc5:
X-ray Structure of c-Met kinase in complex with inhibitor (S)-6-(1-(6- (1-methyl-1H-pyrazol-4-yl)-(1,2,4)triazolo(4,3-b)pyridazin-3-yl)ethyl) quinoline.
Method: X-RAY DIFFRACTION / Resolution: 2.2 Å

PDB-3zcl:
X-ray Structure of c-Met kinase in complex with inhibitor (S)-3-(1-(1H-pyrrolo(2,3-b)pyridin-3-yl)ethyl)-N-isopropyl-(1,2,4)triazolo(4,3- b)pyridazin-6-amine
Method: X-RAY DIFFRACTION / Resolution: 1.4 Å

Chemicals

ChemComp-6XE:
6-[[6-(4-fluorophenyl)-[1,2,4]triazolo[4,3-b][1,2,4]triazin-3-yl]methyl]quinoline

ChemComp-HOH:
WATER

ChemComp-W9Z:
6-{(1S)-1-[6-(1-methyl-1H-pyrazol-4-yl)[1,2,4]triazolo[4,3-b]pyridazin-3-yl]ethyl}quinoline

ChemComp-5TF:
(S)-3-(1-(1H-pyrrolo(2,3-b)pyridin-3-yl)ethyl)-N-isopropyl-(1,2,4)triazolo(4,3-b)pyridazin-6-amine

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / INHIBITOR / KINASE

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