. 2021 May 4;64(9):5429–5446. doi: 10.1021/acs.jmedchem.0c01601

Table 3. Inhibition (Expressed as % of Inhibition at 10 μM or IC₅₀) of Recombinant Human Cytochromes P450 Enzymes and Inhibition of the hERG Channel (Expressed as % of Inhibition at 10 μM).

	cytochrome inhibition^a
	CYP 1A2	CYP 2C9	CYP 2C19 (μM)	CYP 2D6	CYP 3A4^b
Cpd					(BFC)	(DBF)	hERG channel inhibition (% at 10 μM)
20	1 ± 2	17 ± 3	1.9	1 ± 1	2 ± 2	14 ± 1	4
22	14 ± 4	31 ± 3	2.2	11 ± 3	1 ± 2	52 ± 4	44

The cytochrome inhibition was tested at 10 μM. IC₅₀ was calculated for those compounds that presented >50% of inhibition.

For the study of CYP3A4, two different substrates were used: benzyloxytrifluoromethylcoumarin (BFC) and dibenzylfluorescein (DBF).

Table 3. Inhibition (Expressed as % of Inhibition at 10 μM or IC50) of Recombinant Human Cytochromes P450 Enzymes and Inhibition of the hERG Channel (Expressed as % of Inhibition at 10 μM).