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Table 1 Summary of compounds tested, in vitro screening methods, and results

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

Number of compounds Source In vitro testing by: In vitro testing method No. hits (%) No. tested in vivo*
~3,800 • 800 FDA-approved drugs (2008) SJCRH • SYBR® I dye DNA staining assay 24 (0.6) 1
• 2,700 bio-actives (Prestwick, Sigma-Lopac, and MSD)  P. falciparum 3D7 and K1   
• 296 FDA-approved drugs (2009)     
• 47 ‘anti-proliferative’ compounds     
63 GSK discontinued clinical candidates GSK • Whole-cell [3H] hypoxanthine radioisotope incorporation 4 (6.4) 0
P. falciparum 3D7A   
176 Pfizer STLAR library of discontinued clinical candidates Discovery biology • HTS screen using DAPI DNA imaging assay with P. falciparum 3D7 and Dd2 5 (2.8) 1
  Pfizer • EC50 determined using SYBR® I dye DNA staining assay with P. falciparum 3D7 and K1   
100 AstraZeneca discontinued clinical candidates AstraZeneca • SYBR® I dye DNA staining assay 6 (6.0) 2
P. falciparum NF54   
  1. SJCRH, St Jude’s Children’s Research Hospital; FDA, Food and Drug Administration; GSK, GlaxoSmithKline; HTS, high-throughput screening; DAPI, 4′,6-diamidino-2-phenylindole.
  2. *Two additional compounds were sourced for in vivo testing, one each from Novartis and Cephalon Inc. In vivo testing was performed only on those compounds that had an acceptable clinical toxicity/safety/pharmacokinetic profile (or no clinical data). Except for AstraZeneca compounds, which were tested in house, all in vivo testing was performed by GlaxoSmithKline.