Ion Channel

Knowledge and expertise in the field of Ion Channel inhibitors

Libraries designed as voltage gated potassium channel inhibitors (Kv4.3, Kv1.5 & Kv1.3)
The libraries contained >20 novel scaffolds. Screening of 2500 compounds has identified novel hits with IC50s < 30µM (hit rate 6.6%)
Specific rationale employed to enhance the solubility and the metabolic stability of the compounds
Running 2 different hit series through several optimization cycles improving the activity/selectivity profiles, optimizing pharmacokinetic properties, solving identified issues
Having identified 2 compounds as Early Development Candidates (Kv4.3) for the treatment of Atrial Fibrillation