PDBe 5amn

X-ray diffraction
2.57Å resolution

The Discovery of 2-Substituted Phenol Quinazolines as Potent and Selective RET Kinase 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:
homo dimer (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Soluble RET kinase fragment Chain: A
Molecule details ›
Chain: A
Length: 299 amino acids
Theoretical weight: 34.35 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P07949 (Residues: 705-1012; Coverage: 27%)
Gene names: CDHF12, CDHR16, PTC, RET, RET51
Sequence domains: Protein tyrosine kinase
Structure domains:

Ligands and Environments

2 bound ligands:

1 modified residue:

Experiments and Validation Details

Entry percentile scores
X-ray source: DIAMOND BEAMLINE I03
Spacegroup: P43212
Unit cell:
a: 50.57Å b: 50.57Å c: 242.84Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.186 0.183 0.237
Expression system: Spodoptera frugiperda