PDBe 5tq7

X-ray diffraction
2.1Å resolution

Design and Synthesis of a pan-JAK Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin

Released:

Function and Biology Details

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

Structure analysis Details

Assembly composition:
monomeric (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Tyrosine-protein kinase JAK2 Chains: A, B
Molecule details ›
Chains: A, B
Length: 304 amino acids
Theoretical weight: 35.89 KDa
Source organism: Homo sapiens
Expression system: Homo sapiens
UniProt:
  • Canonical: O60674 (Residues: 837-1132; Coverage: 26%)
Gene name: JAK2
Sequence domains: Protein tyrosine kinase

Ligands and Environments

1 bound ligand:

1 modified residue:

Experiments and Validation Details

Entry percentile scores
X-ray source: ALS BEAMLINE 5.0.2
Spacegroup: P21
Unit cell:
a: 37.061Å b: 185.108Å c: 52.492Å
α: 90° β: 110.64° γ: 90°
R-values:
R R work R free
0.229 0.226 0.286
Expression system: Homo sapiens