PDBe 2osc

X-ray diffraction
2.8Å resolution

Synthesis, Structural Analysis, and SAR Studies of Triazine Derivatives as Potent, Selective Tie-2 Inhibitors

Released:

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

Structure analysis Details

Assembly composition:
monomeric (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Angiopoietin-1 receptor Chain: A
Molecule details ›
Chain: A
Length: 317 amino acids
Theoretical weight: 36.25 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
UniProt:
  • Canonical: Q02763 (Residues: 808-1124; Coverage: 29%)
Gene names: TEK, TIE2, VMCM, VMCM1
Sequence domains: Protein tyrosine kinase
Structure domains:

Ligands and Environments

1 bound ligand:

No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: RIGAKU RU200H
Spacegroup: P41212
Unit cell:
a: 62.995Å b: 62.995Å c: 178.814Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.251 0.251 0.306
Expression system: Escherichia coli