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Table 5 Most active compounds in vitro from the AstraZeneca discontinued drugs compound set

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

Compound Target Pf EC50(μM) HepG2 EC50(μM) Status in original indication
AZ-1 Trk1 0.6 10.4 Stopped after GLP toxicity
AZ-2 JAK2 0.1 2.0 Stopped after GLP toxicity
AZ-3 FAR 1.1 11.7 Stopped after Phase II
AZ-4 CDK2 1.2 11.3 Stopped after GLP toxicity
AZ-5 Aurora kinase 1 0.4 17.1 Stopped after GLP toxicity
AZ-6 CHK1 0.4 0.3 Stopped after GLP toxicity
  1. GLP, good laboratory practice.
  2. Study performed by AstraZeneca.
  3. SYBR® I fluorescence assay for activity against P. falciparum strain NF54 and cytotoxicity assay against HepG2.