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. 2018 Nov 5;3(11):14814–14823. doi: 10.1021/acsomega.8b02254

Figure 7.

Figure 7

Screening of structural analogs of ML297 for agonistic activity on GIRK1/2 channels. (a,d) Exemplary DMR (a) and impedance (d) traces of HEK GIRK1/2 cells after addition of 10 μM of a test compound structurally derived from ML297, either in the absence or presence of channel inhibitor SCH. In the following, the test compounds are referred to by the last three digits of their Vanderbilt University code. (b,e) AUCs from (a,d), respectively, and normalized to the indicated concentration of ML297. (c,f) are concentration–response curves derived for hit compounds using the DMR (c) or impedance (f) platform (n = 3). pEC50 values for DMR and impedance were determined as 5.07 ± 0.13; 5.22 ± 0.13 for ML297, 5.50 ± 0.16; 5.82 ± 0.16 for 551, and 5.06 ± 0.11; (too low to determine) for 553.