ONO-2920632

Potency assay (off target): Selectivity was assessed among the K2P family of ion channels as well as a more comprehensive evaluation Eurofins Lead Profiling panel. ONO-2920632 was >150-fold selective against TASK-1, TASK-2, TASK-3, TRAAK and TWIK-2 over TREK-2. The only off-target activity in the K2P family was at TRESK, where 19b showed micromolar inhibitor activity (31-fold selective versus TREK-2).

Potency assay (off target): In the Eurofins Lead Profiling panel of 72 GPCRs, ion channels and transporters, there were no displacements of any radioligand >50% at 30 μM, including the three opiate receptors profiled (DOP, 9%@30 μM, KOP, 8%@30 μM and MOP, 1%@30 μM).