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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.