Figure 1.

ETX001 is a potent and efficacious potentiator of human recombinant TMEM16A (anoctamin-1). (A and C) Whole-cell patch-clamp electrophysiological recordings from Fischer rat thyroid cells stably expressing hTMEM16A in the absence (black lines) and presence (red lines) of primary screening hit (A) and the optimized compound ETX001 (C) at indicated concentrations. Dashed lines indicate the zero-current level. (B and D) Current–voltage relationships for vehicle and indicated concentrations of compounds are shown. (E) Concentration–response curves for the primary screening hit and ETX001. Mean data (±SEM) (screening hit n = 5; ETX001 n = 14) are shown. EC₅₀ = half-maximal effective concentration.