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Structures and activity in fluorometric assays of HC-070 and HC-608.

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posted on 31.01.2018 by Stefan Just, Bertrand L. Chenard, Angelo Ceci, Timothy Strassmaier, Jayhong A. Chong, Nathaniel T. Blair, Randall J. Gallaschun, Donato del Camino, Susan Cantin, Marc D’Amours, Christian Eickmeier, Christopher M. Fanger, Carsten Hecker, David P. Hessler, Bastian Hengerer, Katja S. Kroker, Sam Malekiani, Robert Mihalek, Joseph McLaughlin, Georg Rast, JoAnn Witek, Achim Sauer, Christopher R. Pryce, Magdalene M. Moran

The chemical structures of (A) HC-070 and (B) HC-608 (Pico145). (C) Inhibition of hTRPC5 by HC-070 and HC-608 in indicator-assisted calcium influx analysis. Concentrations tested ranged from 1 picomolar (pM) to 1 μM. Each data point represents the average of 8 measurements from a 384-well plate. Error bars show the standard deviation. The IC50 values were 9.3 ± 0.9 and 6.2 ± 0.5 nanomolar (nM), respectively. (D) Inhibition of hTRPC4 by HC-070 and HC-608 over the same range of concentrations. The IC50 values were 46.0 ± 3.9 nM and 32.5 ± 1.8 nM, respectively (n = 8). Error bars represent the standard deviation.