› 6gqk

X-ray diffraction
2.31Å resolution

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-145426 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Mast/stem cell growth factor receptor Kit Chains: A, B
Molecule details ›
Chains: A, B
Length: 328 amino acids
Theoretical weight: 37.33 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli BL21(DE3)
UniProt:
  • Canonical: P10721 (Residues: 551-687, 771-934; Coverage: 32%)
Gene names: KIT, SCFR
Sequence domains: Protein tyrosine and serine/threonine kinase
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand F88 2 x F88
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: DIAMOND BEAMLINE I04-1
Spacegroup: P212121
Unit cell:
a: 88.19Å b: 91.65Å c: 92.03Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.188 0.187 0.22
Expression system: Escherichia coli BL21(DE3)

Quick links

Citations

3 review citations

1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview.
Bozorov et al. (2019)
2 more

4 mentions without citation

Small Molecule c-KIT Inhibitors for the Treatment of Gastrointestinal Stromal Tumors: A Review on Synthesis, Design Strategies, and Structure-Activity Relationship (SAR).
Godesi et al. (2023)
3 more