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Table 1 IC50 of hERG channel blockers

From: Electrophysiological analysis of mammalian cells expressing hERG using automated 384-well-patch-clamp

Reagents IC50
Data in this study Previous data (References)
Astemizole 6.85 nM (n = 23) 0.9 nM (2), 26 nM (4)
Cisapride 21.2 nM (n = 24) 44 nM (1), 6.9 nM (4), 23-27 nM (5)
E-4031 22.6 nM (n = 30) 18.1 nM (4), 12-17 nM (5)
Quinidine 376 nM (n = 26) 410 nM (3), 820-1,070 nM (5), 750 nM (6)
Terfenadine 41.7 nM (n = 22) 56 nM (1), 6.6-8.4 nM (5), < 52 nM (7)
  1. References for Table 1.
  2. 1. Lacerda AE, et al.: Eur Heart J Supplements 2001, 3:K23-K30.
  3. 2. Zhou Z, et al.: J Cardiovasc Electrophysiol 1999, 10:836-843.
  4. 3. Paul AA, et al.: Br J Pharmacol 2002, 136:717-729.
  5. 4. Chiu PJ, et al.: J Pharmacol Sci 2004, 95:311-319.
  6. 5. Kirsch GE, et al.: J Pharmacol Toxicol Methods 2004, 50:93-101.
  7. 6. Wolpert C, et al.: J Cardiovasc Electrophysiol 2005, 16:54-58.
  8. 7. Katchman AN, et al.: J Pharmacol Exp Ther 2006, 316:1098-1106.