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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.