Table 9.

Cytotoxicity profiling of most potent hits and reference compounds.

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
1a	NA	−2	4	68	92
2a	73	28	39	77	100
3a	96	42	10	94	100
4a	83	75	65	95	85
5f	59	17	14	66	99
6b	100	34	27	62	97
7a	93	62	−9	9.9	58[f]

NA = not applicable;

^[a]CatSper data from Fig. 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.