Table 9.

Ion channel profiling of most potent hits and reference antagonists.

Compound	Inhibition at 10 μM [%]
	CatSper[a]	hSlo3[b]	hCav1.2[c]	hNav1.5[d]	hERG[e]
Dofetilide	NA	NA	NA	NA	IC50= 16 nM[f]
Nifedipine	NA	NA	IC50= 0.13 nM	NA	NA
Verapamil	NA	NA	NA	IC50= 10 μM	NA
1 a	NA	−2	4	68	92
2 a	73	28	39	77	100
3 a	96	42	10	94	100
4 a	83	75	65	95	85
5 f	59	17	14	66	99
6 b	100	34	27	62	97
7 a	93	62	−9	9.9	58[f]

NA=not applicable; [a] CatSper data from Figure 7, n=3 independent experiments; [b] HEK293 cell line stably expressed with hSlo3 and LRRC52, assay performed by manual patch‐clamp, n=5 cells; [c] hCAV1.2 tested in stably expressed cell line using a FLIPR assay protocol, n=2 cells; [d] CHO cell line stably expressing hNAV1.5, assay performed by manual patch‐clamp, n=2 cells; [e] HEK293 cell line stably expressed with hERG gene, assay performed by manual patch‐clamp, n=2 cells; [f] n=2 independent experiments.