Insights That Move the GPCR Field Forward

Signaling bias is critical for drug discovery as it forms a selection criterion for agonism. Measuring and quantifying signaling bias reveals which candidates emphasize therapeutically beneficial pathways, and which may be falsely characterized as equivalent by single-pathway assays. Drug discovery programs that do not consider investigating for signaling bias often fail to fully understand the distinction and risk candidate molecules from advancing along the pipeline.

Nine out of ten GPCR programs stall not because the target was wrong, but because teams waited too long to test the right thing. Terry Kenakin has seen this story play out for 40 years — and he’s rewriting the ending.