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. Author manuscript; available in PMC: 2024 Oct 18.
Published in final edited form as: J Med Chem. 2024 Jul 25;67(15):13033–13055. doi: 10.1021/acs.jmedchem.4c01005

Table 3. Selectivity for PfSUB1 vs proteasome H20S inhibition.

graphic file with name EMS198616-i021.jpg
Entry Cmpd. R2 IC50, nM PfSUB1
inhibition		 IC50, nM H20S
inhibition		 S (H20S vs
PfSUB1
inhibition)
1 1a Ac 5.7±0.228 32.8 ± 1.7 5.7
2 1b Ac 9.3 ± 0.528 35.4 ± 1.7 3.8
3 1c Ac 18.7±1.828 35 640 ± 1 800 1905
4 3a graphic file with name EMS198616-i022.jpg 9.5±0.6 6.0 ± 0.5 0.6
5 4a 36.1±2.4 410 ± 5 11.3
6 3b graphic file with name EMS198616-i023.jpg 9.3±0.2 7.0 ± 0.1 0.75
7 4b 13.0±0.6 160 ± 10 12.3
8 3c graphic file with name EMS198616-i024.jpg 6.9 ±0.3 n.d. n.d.
9 4c 15.3±0.1 1 000 ± 70 65.4
10 5a a - Non inhibitoryb 3-2034
a

Bortezomib control.

b

Bortezomib used at 1 μM does not inhibit rPfSUB1 (see Supporting Information).