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Table 3 Most active compounds in vitro from the GlaxoSmithKline discontinued drugs compound set

From: Repositioning: the fast track to new anti-malarial medicines?

Compound

Class (therapeutic area)

IC50μM

Piritrexim

Dihydrofolate reductase inhibitor (oncology)

0.011 ± 0.001

SB-435495

Phospholipase A2-inhibitor (anti-infective/anti-inflammatory)

1.126 ± 0.146

Lurtotecan

Topoisomerase I inhibitor (oncology)

0.191 ± 0.062

GSK202405

Muscarinic receptor agonist (asthma)

1.582 ± 0.206

  1. Values are mean of three independent measures.
  2. Study performed by GlaxoSmithKline.
  3. IC50 determination against P. falciparum 3D7A strain using [3H] hypoxanthine incorporation assay.