As with other target classes, compound selectivity can be a challenge when targeting ion channels. In particular, compounds often exhibit cross-reactivity between closely related family members. For example, sodium channels have highly conserved extracellular domains, which can hinder the development of compounds that are selective or particular family members, like pain targets Nav1.3 and Nav1.7 versus Nav1.5, a cardiac channel.
Beyond adverse effects related to non-selectivity within a family of ion channels, off-target hits across the ion channelome are also a concern. Many drugs, including those developed against non-ion channel targets, have been shown to interact with hERG, an important cardiac liability target.
Launched in 2005, Eurofins Discovery’s IonChannelProfiler™ services were the first to provide cell-based functional services using automated electrophysiology. High quality and well-characterized PrecisION™ ion channel stable cell lines are the foundation of our IonChannelProfiler™ services. From single-cell manual patch clamp, the gold standard in ion channel work, to high throughput 384-well automated electrophysiology instruments, we use our cells on a variety of platforms to provide the throughput or depth of analysis that matches your needs.
