Broad receptor, enzyme, transporter, and ion channel panel

The Broad receptor, enzyme, transporter, and ion channel panel is a standardized suite of in vitro assays used to assess the secondary pharmacology of drug candidates. It is not a single molecular target but a diagnostic tool comprising dozens of high-risk proteins known to be associated with clinical adverse effects, such as the hERG channel for cardiotoxicity or various GPCRs for central nervous system side effects (Bowes et al., 2012, Nature Reviews Drug Discovery). Pharmaceutical companies utilize these panels to identify off-target binding early in the lead optimization phase, allowing for the engineering of more selective compounds. Results from these panels help in predicting potential toxicities and informing the safety margins for first-in-human studies (Lynch et al., 2017, Expert Opinion on Drug Discovery). Consequently, this panel serves as a gatekeeper in the drug development pipeline to reduce the likelihood of late-stage clinical failure due to safety concerns. By profiling a drug candidate against such a broad array of proteins, researchers can identify unintended interactions that might lead to adverse clinical outcomes or toxicity. This methodological tool is essential for risk assessment rather than being a specific site for therapeutic intervention.

Other names

Safety pharmacology panelOff-target screening panelSecondary pharmacology profiling panelSafety47 panelCerep panelBroad profiling panel

Not applicable as this is a screening panel, not a single therapeutic target.