Table 4Selectivity table showing IC50 (μM) values for ML252 and previously identified KCNQ2 channel blockers for inhibition of a panel of KCNQ channels measured using IonWorks electrophysiology

IC50 (μM)
CompoundKCNQ2KCNQ1KCNQ1/E1KCNQ2/3KCNQ4KCNQ2 (published)a
ML2520.07 ± 0.012.92± 3.908.12± 1.470.12± 0.020.20± 0.06
XE-9910.06 ± 0.010.40± 0.101.60± 0.170.31± 0.110.38± 0.150.71 ± 0.07
UCL20779.42± 1.120.06± 0.020.13± 0.12>3019.29± 11.34.8 ± 0.6
Linopirdine0.71± 0.230.71± 0.282.08± 0.780.92± 0.141.68± 0.311.02
a

IC50’s from published data were taken from [4][5]

From: Identification of a novel, small molecule inhibitor of KCNQ2 channels

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