Presentation: 3A04

Ion channels are an attractive but challenging drug target class. For voltage-gated channels, physiological activity requires voltage control, repetitive stimulation and high temporal resolution. Vertex is utilizing a suite of assay technologies that match these criteria and include the proprietary eVIPR technology, IonWorksHT™ and traditional electrophysiology. eVIPR couples plate-based fluorescence detection with extracellular field stimulation to trigger channel opening enabling a sensitive measure of ion channel state-dependence. IonWorksHT™ is a high throughput voltage clamp system capable of >2000 single cell measurements per day. The combination of these technologies provide robust, reproducible high capacity profiling that are also supported by a parallel cell supply. Thus potency, selectivity and mechanism are measured for >10 ion channel targets which support both diversity library screens and weekly medicinal chemistry. These technologies have enabled the identification of potent and selective state-dependent molecules for Nav and Cav channels that demonstrate in vivo efficacy and safety.

Close Window X