Table 2.

Changes in electrophysiological parameters. For 13 CiPA benchmark drugs, risk categories are shown with changes in APD₉₀ (ΔAPD₉₀), J‐T_peak interval and QT interval observed at IC₅₀ of http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=572. Mexiletine and diltiazem were evaluated at IC₅₀ of I _Na,L and I _Ca,L respectively. Further details can be found in Supporting Information Table S2.1.

Drug name	CiPA risk (Gintant et al. 2016)	I Na IC50[μM]	I Ca,L IC50[μM]	I Kr IC50[μM]	I KsIC50 [μM]	I Na,L IC50[μM]	ETPCunbound[μM]	ΔAPD90 [ms]	QT [ms]	JTpeak [ms]
Quinidine	High	24.79	7.731	0.6377	73.33	‐	3.235	88.580	471	356
Dofetildie	High	124.5	184	0.0098	‐	‐	0.0016	92.645	476	361
Bepridil	High	0.6465	1.455	0.1302	6.0312	‐	0.03463	96.815	478	359
dl‐Sotalol	High	‐	‐	356.4	‐	‐	14.68	93.460	477	359
Terfenadine	Intermediate	0.4798	0.8615	0.0985	‐	‐	0.00029	118.725	484	347
Ondansetron	Intermediate	‐	22.551	1.492	‐	19.181	0.3585	88.660	466	355
Cisapride	Intermediate	2.072	4.278	0.0147	‐	‐	0.002579	92.690	476	361
Chlorpromazine	Intermediate	4.536	8.192	1.118	‐	4.56	0.0345	91.150	474	357
Astemizol	Intermediate	1.862	0.9878	0.0281	‐	‐	0.0002878	92.845	476	361
Ranolazine	Low	41.08	118.3	3.927	‐	26.26	2.31	93.295	474	356
Verapamil	Low	4.272	0.3331	0.2013	29.88	‐	0.08797	89.125	452	344
Mexiletine	Low	‐	‐	‐	‐	8.957	2.5032	‐1.710	342	231
Diltiazem	Low	‐	0.112	6.569	‐	‐	0.1275	33.375	330	230