, 11:P136,
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Date: 09 Nov 2012

The Malaria Box: a catalyst for drug discovery

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The discovery of new chemotypes to feed the pipeline of antimalarial drugs remains a constant challenge, particularly in light of emerging resistance to current therapies. Recently, phenotypic screenings have been successfully used for antimalarial hit generation where the biological target(s) may often not be clearly identified. To catalyse malaria research by both filling the pipeline and having a better understanding of ligand-target relationships, a unique screening tool has been elaborated: the Malaria Box.

The Malaria Box is a set composed of 400 commercially available chemical entities derived from a selection of more than 20,000 hits from the screening of corporate and academic libraries [13]. The originality of the Malaria Box relies in its composition of 200 lead-like and 200 probe-like compounds that have confirmed activity on blood-staged Plasmodium falciparum and that have been assessed for cytotoxicity. Lead-like compounds commensurate with oral absorption and the presenc ...