Multi-kinase panel

A multi-kinase panel is not a single therapeutic target but a collection of protein kinases used to evaluate the potency and selectivity of inhibitors across the human kinome (Nature Reviews Drug Discovery, 2011). These panels typically encompass various kinase families, including receptor tyrosine kinases (RTKs) and serine/threonine kinases, which are critical regulators of signal transduction (UniProt). In drug development, multi-kinase inhibitors such as sorafenib and sunitinib are designed to target multiple proteins within these panels to disrupt complex disease processes like tumor angiogenesis and cell proliferation (PubMed, PMID: 17016431). While targeting multiple kinases can enhance therapeutic efficacy by preventing resistance, it also increases the risk of off-target effects and systemic toxicities (StatPearls, 2023). Consequently, these panels are vital tools for medicinal chemists to optimize the selectivity-score of new chemical entities. The use of such panels helps in identifying potential safety concerns early in the preclinical phase by mapping the drug's interaction profile across hundreds of different enzymes.

Other names

Kinome panelKinase selectivity panelKinase profiling assayMulti-target kinase panel

Simultaneous inhibition of multiple protein kinases (such as VEGFR, PDGFR, and RAF) to disrupt redundant or parallel signaling pathways involved in disease progression (PubMed, PMID: 17016431).