8pqb

X-ray diffraction
1.87Å resolution

c-KIT kinase domain in complex with avapritinib derivative 8

Released:

Function and Biology Details

Reaction catalysed:
ATP + a [protein]-L-tyrosine = ADP + a [protein]-L-tyrosine phosphate
Biochemical function:
Cellular component:
  • not assigned

Structure analysis Details

Assembly composition:
monomeric (preferred)
PDBe Complex ID:
PDB-CPX-145426 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Mast/stem cell growth factor receptor Kit Chain: A
Molecule details ›
Chain: A
Length: 327 amino acids
Theoretical weight: 37.19 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P10721 (Residues: 551-687, 766-934; Coverage: 32%)
  • Best match: P10721-4 (Residues: 47-215)
Gene names: KIT, SCFR
Sequence domains: Protein tyrosine and serine/threonine kinase

Ligands and Environments

1 bound ligand:
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: ESRF BEAMLINE ID23-2
Spacegroup: P3121
Unit cell:
a: 55.67Å b: 55.67Å c: 186.08Å
α: 90° β: 90° γ: 120°
R-values:
R R work R free
0.2 0.198 0.234
Expression system: Escherichia coli BL21(DE3)