. 2023 Jun 22;14:3737. doi: 10.1038/s41467-023-39444-y

Table 1.

Biochemical characterization of 1–10, controls 11, 12, auranofin (AF), praziquantel (PZQ), meclonazepam (MZM) and photoreactive probe (PRP)

	ID	S. mansoni TGR IC₅₀ (µM)^a	S. mansoni TGR inhibition (%) at 66.7 µM^b	Human TrxR1 IC₅₀ (µM)^a	Human TrxR1 IC₅₀ (µM) or inhibition (%) at 66.7 µM^b	Human GR (inhibition at 66.7 µM)	Decrease (%) in GSH/GSSG ratio^c
Slow TGR inhibitors	1	>66.7	42.1%	>66.7	37.0 ± 3.44	n.i.	75
	2	>66.7	28.7%	>66.7	50.0 ± 13.6	n.i.	39
	3	>66.7	45.0%	>66.7	42.7 ± 3.95	n.i.	62
	4	>66.7	68.6%	>66.7	19.0 ± 5.72	n.i.	60
	5	>66.7	73.0%	>66.7	28.5%	n.i.	56
Fast TGR inhibitors	6	2.5 ± 0.51	—	>66.7	28.9%	n.i.	32
	7	14.6 ± 1.22	—	22.3 ± 2.03	—	n.i.	38
	8	10.3 ± 2.01	—	4.9 ± 1.72	—	n.i.	20
	9	57.5 ± 2.46	—	70.5 ± 11.4	—	n.i.	9
	10	18.6 ± 2.48	—	13.4 ± 2.0	—	n.i.	n.d.^d
Control	11	n.i.^e	n.i.^e	n. d.^d	n.d.^d	n.i.	0.4
Control	12	n.i.^e	n.i.^e	>66.7	28.6%	n.i.	1.7
	PRP^f	34.9 ± 6.11	—	n.d.^d	n.d.^d	n.d.^d	n.d.^d
	AF	0.007	—	0.02	—	n.d.^d	91
	PZQ	—	n.i.^e	—	n.i.^e	n.d.^d	1
	MZM	—	n.i.^e	—	n.i.^e	n.d.^d	1

Data are represented by n = 3 independent experiments as mean ± SD. Source data are provided as a Source Data file.

^aIC₅₀ after 15 min preincubation (enzyme + 100 µM NADPH + compound).

^bIC₅₀ (µM) or inhibition (%) at 66.7 µM (enzyme + 100 µM NADPH + compound) after 6 h preincubation. Inhibition (%) of TGR activity after 6 h incubation are given and not IC₅₀s because equilibrium between enzyme and inhibitor was not obtained in this time frame (Fig. 3d).

^cratio of GSH/GSSG in adult worms determined after 3 h exposure to compounds at 50 μM.

^dn.d. not determined.

^en.i. no inhibition at 67 μM in 6 h.

^fPRP is a “slow” inhibitor.