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. Author manuscript; available in PMC: 2010 Jun 10.
Published in final edited form as: Infect Disord Drug Targets. 2010 Jun;10(3):226–239. doi: 10.2174/187152610791163336

Table 1.

Representative early hits derived from HTS and medicinal chemistry programs

compound PfDHODH
(IC50) µM		 Human DHODH
(IC50) µM		 Fold selectivity
4 0.016 200 12,500
5 0.23 110 500
6 0.05 >50 >1000
7 0.047 >200 >4000
8 0.042 >30 >700
9 0.34 >30 >90
10 0.083 >30 >360
11 0.93 >30 >30
12 0.16 30 >190

Compounds 4–11 were assayed at the following conditions: CoQD = 20 µM;DHO = 200 µM, DCIP = 100–120 µM, [DHODH] = 10 nM;4–6[72], 7 [73], 8–11 [75];compound 12, conditions were instead: CoQD = 100 µM;DHO = 200 µM, DCIP = 60 µM, [DHODH] = 5 nM [78].