› 8xz7

X-ray diffraction
1.75Å resolution

FGFR1 kinase domain with a covalent inhibitor 10h

Released:
DOI: 10.2210/pdb8xz7/pdb
PDB entry 8xz7 coloured by chain, front view.
PDB entry 8xz7 coloured by chain, side view.
PDB entry 8xz7 coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Design, synthesis and biological evaluation of 5-amino-1H-pyrazole-4-carboxamide derivatives as pan-FGFR covalent inhibitors.
Deng W, Chen X, Liang H, Song X, Xiang S, Guo J, Tu Z, Zhou Y, Chen Y, Lu X
Eur J Med Chem 275 116558 (2024)
PMID: 38870833

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)
Assembly name:
PDBe Complex ID:
PDB-CPX-145801 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Fibroblast growth factor receptor 1 Chains: A, B
Molecule details ›
Chains: A, B
Length: 310 amino acids
Theoretical weight: 35.26 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli #1/H766
UniProt:
  • Canonical: P11362 (Residues: 458-765; Coverage: 39%)
Gene names: BFGFR, CEK, FGFBR, FGFR1, FLG, FLT2, HBGFR
Sequence domains: Protein tyrosine and serine/threonine kinase

Ligands and Environments

2 bound ligands:
Ligand SO4 5 x SO4
Ligand A1LWW 2 x A1LWW
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SSRF BEAMLINE BL10U2
Spacegroup: C2
Unit cell:
a: 210.34Å b: 49.63Å c: 66.74Å
α: 90° β: 106.94° γ: 90°
R-values:
R R work R free
0.188 0.186 0.225
Expression system: Escherichia coli #1/H766

Quick links