Table 3. Immucillin Inhibitors of TcHGXPRT, TcHGPRT, and PfHGXPRT^a.

Inhibitor	TcHGXPRT (app Ki μM)	TcHGPRTb(app Ki μM)	PfHGXPRTb(app Ki μM)
(S)-1	0.6 ± 0.1	0.006 ± 0.002	0.0005 ± 0.00005c
(S)-2	1.6 ± 0.1	0.004 ± 0.002	0.0006 ± 0.00004
(R)-2	38 ± 4	0.5 ± 0.03	0.023 ± 0.002
(S)-3	5.4 ± 0.3	0.017 ± 0.002	0.0012 ± 0.0001
(S)-4	0.7 ± 0.1	1.4 ± 0.03	0.11 ± 0.03
(S)-5	0.9 ± 0.1	13.4 ± 0.9	8 ± 0.5
(±)-6	11 ± 1	0.17 ± 0.02	0.009 ± 0.0001
(±)-7	35 ± 3	1.1 ± 0.2	0.015 ± 0.004c
ImmHP (8)	16 ± 1	0.17 ± 0.03	0.001 ± 0.0003
ImmGP (9)	36 ± 5	1.1 ± 0.4	0.014 ± 0.002
ImmXP (10)	0.20 ± 0.02	36.7 ± 0.7	>100
11	8.4 ± 0.3	0.7 ± 0.2	0.06 ± 0.003
12	8 ± 1	3.6 ± 0.3	0.11 ± 0.006

^aTcHGXPRT assays were performed at 37 °C (pH 8.3) in the presence of 12 mM MgCl₂ and 100 μM PPi. Concentration–response data was fit to eq 11, and K_i values were calculated using eq 12.

^bGlockzin et al., 2022.⁴³

^cGai et al., 2022.⁷⁹