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By means of a custom-developed automated patch clamp protocol, a library of 6-substituted and 56-disubstituted amiloride analogs was screened. The outcome of this work was the identification of 6-iodoamiloride as a potent ASIC1 inhibitor. Follow-up IC50 assays in tsA-201 cells corroborated the superior inhibitory effect of 6-iodoamiloride on ASIC1, manifesting as an IC50 of 88 nM for hASIC1 94. Amiloride's IC50 w