› 3zcl

X-ray diffraction
1.4Å resolution

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

Released:
DOI: 10.2210/pdb3zcl/pdb
PDB entry 3zcl coloured by chain, front view.
PDB entry 3zcl coloured by chain, side view.
PDB entry 3zcl coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Lessons 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.
Cui JJ, Shen H, Tran-Dubé M, Nambu M, McTigue M, Grodsky N, Ryan K, Yamazaki S, Aguirre S, Parker M, Li Q, Zou H, Christensen J
J Med Chem 56 6651-65 (2013)
PMID: 23944843

Function and Biology Details

Reaction catalysed: 
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
Biochemical function:
Biological process:
Cellular component:
  • not assigned
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-140186 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Hepatocyte growth factor receptor Chain: A
Molecule details ›
Chain: A
Length: 306 amino acids
Theoretical weight: 34.88 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P08581 (Residues: 1051-1348; Coverage: 22%)
Gene name: MET
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand 5TF 1 x 5TF
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 5.0.2
Spacegroup: P21212
Unit cell:
a: 76.997Å b: 94.509Å c: 46.834Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.194 0.193 0.211
Expression system: Spodoptera frugiperda

Quick links

Citations

3 review citations

The Function of the HGF/c-Met Axis in Hepatocellular Carcinoma.
Wang et al. (2020)
2 more

4 mentions without citation

The azaindole framework in the design of kinase inhibitors.
Mérour et al. (2014)
3 more