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. Author manuscript; available in PMC: 2024 May 18.
Published in final edited form as: Cell Chem Biol. 2023 May 5;30(5):457–469.e11. doi: 10.1016/j.chembiol.2023.04.006

Table 1.

Proteasome inhibition activity and Plasmodium growth inhibition of ATZs and their constituent pharmacophores

ID IC50 (nM)
EC50 (nM)
Pf20S Hu i-20S Hu c-20S Pf Dd2WT Dd2β6A117D Dd2β5A49S HepG2

ART1 9,200 ± 720 >100,000 >100,000 43.7 ± 12.7 27.9 ± 11.0 30.2 ± 2.6 >100,000
PI01 6.0 ± 0.8 200 ± 46 2,000 ± 240 7.4 ± 0.2 121 ± 20 >2,770 >100,000
ATZ2 2.9 ± 0.6 73 ± 19 210 ± 40 3.0 ± 0.6 4.4 ± 1.1 10.9 ± 2.6 5,800 ± 620
ATZ4 4.3 ± 0.9 200 ± 57 890±140 4.3 ± 1.3 6.7 ± 2.2 5.9 ± 1.9 9,400 ± 1,700
Deoxy-ATZ4 4.4 ± 0.5 300 ± 22 1100 ± 46 21.6 ± 1.4 246.0 ± 44.5 >2,770 10,800 ± 500

All data are means of at least three independent experiments and are presented with standard deviation. Data were rounded to three or fewer significant figures.