› 2wd1

X-ray diffraction
2Å resolution

Human c-Met Kinase in complex with azaindole inhibitor

Released:
DOI: 10.2210/pdb2wd1/pdb
PDB entry 2wd1 coloured by chain, front view.
PDB entry 2wd1 coloured by chain, side view.
PDB entry 2wd1 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Discovery of 4-azaindoles as novel inhibitors of c-Met kinase.
Porter J, Lumb S, Franklin RJ, Gascon-Simorte JM, Calmiano M, Riche KL, Lallemand B, Keyaerts J, Edwards H, Maloney A, Delgado J, King L, Foley A, Lecomte F, Reuberson J, Meier C, Batchelor M
Bioorg Med Chem Lett 19 2780-4 (2009)
PMID: 19369077

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: 292 amino acids
Theoretical weight: 33.05 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P08581 (Residues: 1055-1346; Coverage: 21%)
Gene name: MET
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

2 bound ligands:
Ligand ZZY 1 x ZZY
Ligand GBL 2 x GBL
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SLS BEAMLINE X06SA
Spacegroup: P21
Unit cell:
a: 37.411Å b: 42.312Å c: 84.826Å
α: 90° β: 93.01° γ: 90°
R-values:
R R work R free
0.212 0.21 0.265
Expression system: Spodoptera frugiperda

Quick links

Citations

1 review citation

Small molecule c-Met kinase inhibitors: a review of recent patents.
Porter J. (2010)
13 other articles

9 mentions without citation

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