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. Author manuscript; available in PMC: 2012 Nov 10.
Published in final edited form as: J Med Chem. 2011 Oct 10;54(21):7477–7485. doi: 10.1021/jm2005546

Table 2.

Summary of ion channel activity with the three major scaffold types

EC50 (µM) IC50 (µM)

hNav1.5
Compound 3D7 K1 hERG tonic phasic Kir6.2/SUR2A TI (hERG IC50/
K1 EC50)
propafenone 2.69 0.92 2.88 3.3 >5 2.2 3
6z 0.06 0.10 2.6 N/A N/A N/A 26
6ch 0.13 0.005 4.84 >5 >5 >5 895
6k 0.39 0.18 4.31 >5 >5 >5 23
6b 0.09 0.05 3.46 >5 >5 >5 65