› 3a4p

X-ray diffraction
2.54Å resolution

human c-MET kinase domain complexed with 6-benzyloxyquinoline inhibitor

Released:
DOI: 10.2210/pdb3a4p/pdb
PDB entry 3a4p coloured by chain, front view.
PDB entry 3a4p coloured by chain, side view.
PDB entry 3a4p coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.
Nishii H, Chiba T, Morikami K, Fukami TA, Sakamoto H, Ko K, Koyano H
Bioorg Med Chem Lett 20 1405-9 (2010)
PMID: 20093027

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: 319 amino acids
Theoretical weight: 35.99 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P08581 (Residues: 1049-1360; Coverage: 23%)
Gene name: MET
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

3 bound ligands:
Ligand CL 1 x CL
Ligand IPA 2 x IPA
Ligand DFQ 1 x DFQ
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: PHOTON FACTORY BEAMLINE BL-5A
Spacegroup: C2
Unit cell:
a: 157.227Å b: 42.733Å c: 46.039Å
α: 90° β: 102.91° γ: 90°
R-values:
R R work R free
0.186 0.183 0.24
Expression system: Spodoptera frugiperda

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Citations

1 review citation

Quinoline-Based Molecules Targeting c-Met, EGF, and VEGF Receptors and the Proteins Involved in Related Carcinogenic Pathways.
Martorana et al. (2020)
17 other articles

3 mentions without citation

Pre-calculated protein structure alignments at the RCSB PDB website.
Prlic et al. (2010)
2 more