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. Author manuscript; available in PMC: 2009 Jun 26.
Published in final edited form as: J Med Chem. 2008 Jun 4;51(12):3649–3653. doi: 10.1021/jm8001026

Figure 3.

Figure 3

Selective and potent inhibition of PfDHODH and P. falciparum cells by compound 7. A. Inhibition profile for PfDHODH (orange circles; IC50 0.047 ± 0.022 μM; n=6) compared to human DHODH (black diamonds; IC50 >200 μM); [E]T = 10 nM. B. Activity in whole cell assays against P. falciparum 3D7 (orange circles) or mouse L1210 (black diamonds) cells (EC50 = 0.079 ±0.045; n=9). C. Relationship between IC50 and substrate concentration ([E]T = 5 nM). KI was determined by fitting the data to Eq. 2 (KI = 0.015 ± 0.0011 μM). D. Rapid kinetic analysis showing compound 7 inhibits the CoQD-dependent oxidative half-reaction (bottom panel) but not the DHO-dependent reductive half-reaction (top panel). Blue trace (1) - no compound 7 and orange trace (2) - compound 7 (50 μM).