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. 2016 Mar 2;6:22451. doi: 10.1038/srep22451

Table 2. Selected hits.

Pubchem name Compound GUS activity[S/B] optimal conc.for GUS [μg/ml] Viability IC50[μg/ml]
  cis-aconitate 58.3 10 >20
STOCK4S-04391 DIP-01 7.6 50 57.2
STOCK1S-31919 DIP-02 4.2 1.25 1.0
STOCK1S-42137 DIP-03 3.3 0.5 0.3
STOCK1S-13735 DIP-04 8.1 50 25.8
STOCK4S-90544 DIP-05 3.3 12.5 7.7
STOCK3S-11937 DIP-06 4.6 6.3 1.3
STOCK5S-42531 DIP-07 3.8 2.5 2.2
STOCK5S-38263 DIP-08 3.5 12.5 5.5
STOCK5S-44766 DIP-09 3.2 50 16.4
STOCK5S-82907 DIP-10 4.4 3.0 1.7
STOCK5S-91387 DIP-11 3.6 12.5 5.8
STOCK5S-83458 DIP-12 3.1 12.5 10.0
STOCK6S-01740 DIP-13 5.4 75 13.4
STOCK6S-10803 DIP-14 3.3 50 22.5
STOCK6S-14165 DIP-15 5.1 25 9.5
STOCK6S-12339 DIP-16 3.4 12.5 8.8
STOCK6S-10284 DIP-17 3.0 28.1 13.9
STOCK6S-06338 DIP-18 3.6 12.5 6.3
STOCK6S-38758 DIP-19 4.4 1.25 0.8
STOCK6S-34290 DIP-20 3.3 10.9 8.6
STOCK6S-35180 DIP-21 3.4 6.3 4.2
5740240 DIP-22 5.0 9.4 4.6
5742784 DIP-23 3.7 21.9 13.9
T5700438 DIP-24 3.5 3.9 2.3
T6214849 DIP-25 3.4 10.9 6.7
T5314847 DIP-26 5.1 10.9 5.3
T5845297 DIP-27 3.0 9.7 4.6
T5227647 DIP-28 3.9 20 10.9
  Melarsoprol 2.1 0.023 0.016
  Pentamidine 1.0 NA 0.006
  Suramin 1.0 NA 0.08
  Nifurtimox 1.0 NA 1.0
  Fexinidazole 1.0 NA 2.4

GUS activity S/B = ratio of GUS signal of drug-treated samples to untreated (background), at the optimal concentration for GUS activity, IC50: inhibitory concentration resulting in 50% parasite death. NA: not applicable (there was no GUS signal). Each control compound was tested over a ≥1,000 fold concentration range in both assays with the IC50 approximately in the middle of the range. All assays were performed with an exposure time of 40 h; the initial parasite density was 5 × 105/ml in both assays. STOCK5S-42531 is desloratidine.