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 |