8E1X: FGFR2 kinase domain in complex with a Pyrazolo[1,5-a]pyrimidine analog (Compound 29)
X-ray · 2.68 Å · released 23 Nov 2022 · Homo sapiens
Ligand: U9P
How it was solved
- Method
- X-ray
- Resolution
- 2.68 Å
- Released
- 23 Nov 2022
- Rfree
- 0.272
- Rwork
- 0.224
- Clashscore
- 6.16
- Ramachandran outliers
- 0.00%
- Rotamer outliers
- 0.00%
Crystallisation
- Technique
- Vapor Diffusion, Sitting Drop
- pH
- 5.2
- Temperature
- 293.0 K
0.1 M Sodium citrate pH 5.2; 28% w/w PEG 4,000; 0.2 M Ammonium acetate
What it led to
2022 – Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant FGFR2/3
Casebook · 11 Aug 2025
Primary citation
Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3
Journal of Medicinal Chemistry 2022
FGFR2 is the target of 4 approved drugs in ChEMBL.
Do it yourself
Field Guide: Xray and crystallisation
Unlocking Membrane Protein Structures: The Crystallization Revolution Reshaping Drug Discovery
Engineering Protein Stability: Unlocking the Secrets of Successful Crystallization
AXIS: Closing the Loop on Crystal Detection
Playbook
The Self-Driving Lab: How Automation and AI Are Redefining the Pace of Discovery
Tools
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