RESOURCES

How much of your compound’s activity are your assays really detecting? Understanding how receptor density impacts pharmacological responses is critical for accurately characterizing compound activity & identifying candidates with the highest likelihood of therapeutic success. Review the latest GPCR white paper, “Functional ‘Volume Control’ in Cell Systems,” by GPCR expert Terry Kenakin, Ph.D., Professor of Pharmacology at the University of North Carolina School of Medicine, in collaboration with Eurofins DiscoverX^®. The white paper explores how tuning receptor density & system sensitivity can uncover hidden efficacies, improve characterization of agonists & antagonists, & provide more predictive pharmacology.

End-to-End Characterization of a WEE1–CRBN: DDB1 Molecular Glue Ternary Complex

Clinical attrition of drug candidates is frequently driven by unforeseen safety liabilities, which are often associated with off-target pharmacological interactions.

Secondary pharmacology is increasingly used to identify off-target activities with potential clinical safety relevance.

Suzetrigine, the first FDA-approved non-opioid analgesic targeting hNav1.8, marks a pivotal moment in the evolution of pain therapeutics.

Secondary pharmacology identifies off-target interactions that may drive undesirable clinical effects, supporting lead optimization, candidate selection for early risk assessment

In early drug discovery, Caco-2 cells are widely used to estimate intestinal permeability.

Many kinase inhibitor programs face the same obstacle.

For Translational Insights in Metabolic Discovery and Development

Accelerate innovation with complete kinase solutions

Neurotoxicity is a major cause of drug attrition with central nervous system (CNS) affected the most.

Class B GPCR Target Significance