› 4zsa

X-ray diffraction
2Å resolution

Crystal structure of FGFR1 kinase domain in complex with 7n

Released:
DOI: 10.2210/pdb4zsa/pdb
PDB entry 4zsa coloured by chain, front view.
PDB entry 4zsa coloured by chain, side view.
PDB entry 4zsa coloured by chain, top view.
Source organism: Homo sapiens
Primary publication:
Design, synthesis and biological evaluation of novel FGFR inhibitors bearing an indazole scaffold.
Liu J, Peng X, Dai Y, Zhang W, Ren S, Ai J, Geng M, Li Y
Org Biomol Chem 13 7643-54 (2015)
PMID: 26080733

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-145801 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Fibroblast growth factor receptor 1 Chains: A, B
Molecule details ›
Chains: A, B
Length: 308 amino acids
Theoretical weight: 35.08 KDa
Source organism: Homo sapiens
Expression system: Escherichia coli
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
Structure domains:

Ligands and Environments

1 bound ligand:
Ligand 4UT 2 x 4UT
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: SSRF BEAMLINE BL17U
Spacegroup: C2
Unit cell:
a: 209.91Å b: 57.181Å c: 65.55Å
α: 90° β: 107.47° γ: 90°
R-values:
R R work R free
0.206 0.204 0.254
Expression system: Escherichia coli

Quick links

Citations

5 review citations

Epigenetic polypharmacology: A new frontier for epi-drug discovery.
Tomaselli et al. (2020)
4 more

4 mentions without citation

Current progress, challenges and future prospects of indazoles as protein kinase inhibitors for the treatment of cancer.
Tandon et al. (2021)
3 more