› 3f66

X-ray diffraction
1.4Å resolution

Human c-Met Kinase in complex with quinoxaline inhibitor

Released:
DOI: 10.2210/pdb3f66/pdb
PDB entry 3f66 coloured by chain, front view.
PDB entry 3f66 coloured by chain, side view.
PDB entry 3f66 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Discovery of a novel series of quinoxalines as inhibitors of c-Met kinase.
Porter J, Lumb S, Lecomte F, Reuberson J, Foley A, Calmiano M, le Riche K, Edwards H, Delgado J, Franklin RJ, Gascon-Simorte JM, Maloney A, Meier C, Batchelor M
Bioorg Med Chem Lett 19 397-400 (2009)
PMID: 19059779

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 Chains: A, B
Molecule details ›
Chains: A, B
Length: 298 amino acids
Theoretical weight: 33.85 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P08581 (Residues: 1052-1349; Coverage: 22%)
Gene name: MET
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

3 bound ligands:
Ligand IHX 2 x IHX
Ligand GBL 5 x GBL
Ligand NA 1 x NA
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SLS BEAMLINE X06SA
Spacegroup: P1
Unit cell:
a: 47.377Å b: 47.587Å c: 75.6Å
α: 100.7° β: 103.62° γ: 98.29°
R-values:
R R work R free
0.168 0.168 0.225
Expression system: Spodoptera frugiperda

Quick links

Citations

5 review citations

Small molecule c-Met kinase inhibitors: a review of recent patents.
Porter J. (2010)
4 more

8 mentions without citation

A novel mechanism by which small molecule inhibitors induce the DFG flip in Aurora A.
Martin et al. (2012)
7 more