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Table 4 Most active compounds in vitro from the Pfizer STLAR library

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

Compound Class (therapeutic area) EC503D7 (μM) EC50K1 (μM)
UK-112,214 Dual platelet activating factor/histamine H1 receptor antagonist (allergic rhinitis) 0.55 (0.45, 0.65) 0.6 (NA)
CP-631992 Neuropeptide Y5 receptor antagonist (obesity) 0.7 (NA) 0.40 (0.2, 0.6)
CE-245677 TIE2 tyrosine kinase inhibitor (oncology) 1.1 (NA) 0.8 (NA)
CJ-0231112 Bradykinin B2 receptor antagonist (pain) 0.65 (0.36, 0.94) 0.4 (NA)
AG-024322 CDK1/2/4/5 inhibitor (oncology) 0.7 (0.11, 1.29) 0.4 (NA)
  1. NA, not available. EC50 values are shown as mean (95% CI). Compounds with an EC50 < 1 μM against either P. falciparum strain are shown.
  2. Study performed by Pfizer Inc.
  3. SYBR® I fluorescence assay for activity against P. falciparum strains 3D7 and K1.