GPCR Safety Panels Launched

We are pleased to introduce our new GPCR Safety Panels, designed to help evaluate the off-target potency of candidate compounds in drug discovery and preclinical research. These panels include G-protein coupled receptors (GPCRs) often linked with common adverse reactions, making them practical resources for pharmaceutical R&D.

Our standard GPCR Safety Panel features a minimal set of 24 representative GPCRs, allowing for testing compounds in agonistic and antagonistic modes. For broader coverage, the GPCR Safety Panel Premium exhaustively includes 31 additional GPCRs from the same receptor families. The list of the receptors in the panels can be found at the bottom of this page.

Several GPCR families are known to cause common adverse reactions when activated or inhibited (Nat Rev Drug Discov. 11:909-22). To name but a few, agonism of muscarinic acetylcholine receptors may induce convulsions and hypertension, and antagonism of endothelin receptors is potentially teratogenic. Thus, understanding these off-target interactions is critical to ensuring the development path, and pharmaceutical researchers routinely screen them. Our GPCR Safety Panels aim to comprehensively assess these potential off-target interactions, helping pharmaceutical companies ensure the safety of their candidate molecules.

Key Advantages of Our GPCR Safety Panels

Early Identification of Off-Target Interactions

Our panels allow for the early detection of off-target interactions at the lead selection stage. This early detection is crucial for mitigating unwanted activities through structure-activity relationship (SAR) studies, thereby enhancing the safety profile of candidate compounds.

Predictive Insights into Clinical Adverse Reactions

GPCR Safety Panels offer predictive insights into clinical adverse reactions that may go unnoticed through in vivo studies. For instance, they can predict valvulopathy associated with 5-hydroxytryptamine receptor 2B (HTR2B) agonists. Furthermore, our panels use human GPCRs, which correlate better with clinical adverse effects in humans than animal orthologs.

Cost-Effective In Vitro Testing

A large number of compounds can be tested cost-effectively in vitro on human targets associated with clinical adverse drug reactions. This efficiency is invaluable for screening representative chemical series in the early stages of drug discovery, facilitating the identification of the best leads.

Relevance to Physiology

Unlike traditional binding assays, our proprietary GPCR functional assay measures the potency of test compounds against GPCRs. This provides information more relevant to physiology, offering insights closely aligned with clinical implications.

Accelerated Research Timeline

GPCR Safety Panels enable quicker acquisition of results and potential explanations of off-target effects compared to in vivo studies. This acceleration allows for efficient integration of data from safety pharmacology profiling, pharmacokinetic experiments, ADME (absorption, distribution, metabolism, and excretion), and efficacy models, forming an early safety risk assessment.

Flexibility for Streamlined Research

Our GPCR collection covers a total of 550 human receptors and mouse orthologues. In addition, we offer the flexibility to prepare orthologues for other species commonly used in preclinical studies, such as rats, dogs, rabbits, and macaques. This adaptability ensures you can customize our panel to suit your research needs, reducing delays and reliance on animal models while maintaining data integrity.

Competitive Benchmarking

Data from GPCR Safety Panelsl help benchmark against competitor compounds, supporting the development of a best-in-class strategy. By addressing pharmacological promiscuity early on, we help ensure that compounds entering development have minimal or no off-target activities.

Conclusion

Our GPCR Safety Panels significantly advancedrug discovery and preclinical research. Providing detailed and relevant data on off-target interactions empowers pharmaceutical researchers to make informed decisions, optimize candidate selection, and enhance the safety and efficacy of new drugs. We invite you to explore the potential of our GPCR Safety Panels and join us in revolutionizing drug discovery and preclinical research. For more information on our GPCR Safety Panels or to schedule a consultation, please get in touch with our team via the inquiry form. We look forward to collaborating with you on your next groundbreaking project.

Panel Receptors