Over 5 million compounds screened

Data from three projects released into the public domain

03 May 2010

In its search for new molecules against malaria, MMV and partners have so far supported the screening of more than 5 million compounds for their potential activity against the malaria parasite. Three partners of the MMV-supported early discovery projects have gone a step further and released the data pertaining to the active molecules into the public domain. This bold move will enable scientists the world over to access these data ensuring their antimalarial potential be used to the full.

GlaxoSmithKline (GSK), have worked to screen more than 2 million compounds from their in-house library for activity against Plasmodium falciparum – the most prevalent strain of malaria parasite in Africa. The screen resulted in the identification of more than 13,500 compounds with activity against the parasite. The largest group of compounds with a known mode of action to be identified was the kinase inhibitors, which are currently being explored in two other MMV-supported projects: GSK miniportfolio and Monash University’s Kinase Platform.

The Genomics Institute of the Novartis Research Foundation has screened more than 800,000 compounds, from a range of sources, resulting in more than 5,600 molecules active against the parasite. Four of these chemical series have been selected for further development at Novartis Institute of Tropical Diseases (NITD). One series is now undergoing candidate selection for clinical trials, while the other three are in lead optimization.

The team from St Jude Children’s Research Hospital has screened more than 300,000 unique chemical structures also against P. falciparum, yielding over 1,100 potent and selective drug discovery starting points. In collaboration with Rutgers University in New Jersey the team at St Jude is working to take these starting points to the next level.

These projects bring the total number of promising compounds to over 20,000.

Data from GSK and St Jude’s screening work has been published in Nature, while all data, including those of Novartis, can be found online through the European Bioinformatics Institute (EMBL-EBI). Sharing these data will not only expedite the discovery and development of future antimalarials it has also set a precedent for other actors in neglected disease drug discovery to follow the open access model.