Case Study: How XtalPi Used Diversity Library of 80K Compounds to Find Hits Targeting FGFR3 

Mutations in Fibroblast Growth Factor Receptor 3 (FGFR3) are linked to various cancers, making it a critical target for therapeutic intervention. But targeting specific FGFR members individually is very challenging due to their structural similarities. Currently only pan-inhibitors are approved by the FDA.

In an effort to selectively target FGFR3, XtalPi sought to identify novel scaffolds using our curated high-throughput screening (HTS) diversity library.

Our Key Results:

• Discovery of 15 potent hit compounds, each exhibiting biochemical potency with IC₅₀ values below 10 μM.
• Identified three hit series which possessed novel scaffolds that are distinct from those of known FGFR3 inhibitors, providing new avenues for selectively targeting the protein.