Figure 1.
High-throughput screen of ion-channel modulators. (A) General sulfonamide motif. (B) Example of a biaryl sulfonamide motif. (C) The voltage protocol used in in the high-throughput screen together with a representative effect of an ion-channel opening compound on the current. (D) Summary of data from almost 18,000 compounds tested on the 3R Shaker KV channel expressed in CHO cells. Ion currents were recorded by IonWorks (see Materials and methods) and measured at the end of a 150-ms-long voltage-clamp step to +10 mV. Holding voltage, −80 mV. The data points are aligned in potency order. The gray area indicates no effect, the dashed and dotted lines define clear openers (243 compounds, 1.3% of all tested compounds) or clear blockers (140 compounds, 0.8% of all tested compounds; see text for a detailed description).