ML-365 is a bis-amide TASK-1 potassium channel blocker (IC50 = 16 nM).1 It is selective for TASK-1 over TASK-3 channels in a QPatch assay (IC50 = 990 nM). It also acts as an antagonist of the metabotropic glutamate receptor mGluR5 (IC50 = 1.35 μM).2
1.Flaherty, D.P., Simpson, D.S., Miller, M., et al.Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffoldBioorg. Med. Chem. Lett.24(16)3968-3973(2014) 2.Zhou, Y., Rodriguez, A.L., Williams, R., et al.Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTSBioorg. Med. Chem. Lett.19(23)6502-6506(2009)