Ion channels represent 15 – 20% of historic drug approvals and recent drug discovery projects. Many ion channel families (Nav, Cav, TRPx and GABA) are validated as therapeutic targets based on human genetics, animal models and selective pharmacology. However, ion channels are challenging targets requiring specialist target class knowledge and screening technology such as automated patch clamp (APC) electrophysiology.
Here we outline our example where a pharma company interested in ion channels, but lacking expertise and screening platforms turned to a specialist CRO to fill this knowledge gap. In our case a Japanese pharma company with plate-based assay data wanted to expand medicinal chemistry SAR by accessing high quality APC and ion channel expertise.
During the collaboration selective Kv1.3 modulators with nM potency and efficacy against human T-cells were identified.