PDBe 3emg

X-ray diffraction
2.6Å resolution

Discovery and SAR of novel 4-thiazolyl-2-phenylaminopyrimidines as potent inhibitors of spleen tyrosine kinase (SYK)

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:
Tyrosine-protein kinase SYK Chain: A
Molecule details ›
Chain: A
Length: 291 amino acids
Theoretical weight: 33.71 KDa
Source organism: Homo sapiens
Expression system: Spodoptera frugiperda
UniProt:
  • Canonical: P43405 (Residues: 349-635; Coverage: 45%)
Gene name: SYK
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: ALS BEAMLINE 5.0.2
Spacegroup: P21
Unit cell:
a: 39.87Å b: 84.45Å c: 41.44Å
α: 90° β: 99.63° γ: 90°
R-values:
R R work R free
0.2 0.2 0.222
Expression system: Spodoptera frugiperda