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Primary screening studies initially generate a list of compounds with the required biological activities (‘Hits’). These Hits rarely fulfil all the criteria for a quality 'tool' compound as they typically show only a moderate affinity for the target and restricted selectivity.
To become a useful tool compound, the chemical properties of the initial Hits must therefore be iteratively improved by suitable structural modification. The post-screening Hit-to-tool optimisation process is carried out by accredited chemistry partner sites in EU-OPENSCREEN ERIC Member countries and is organised as a research collaboration between the assay provider and the respective chemistry site.
Currently, the European Commission offers project funding for medicinal chemistry support in our EU-OPENSCREEN ERIC partner sites through the ISIDORe project. Read more here.
Dr. Kamil Paruch
Dr. Marc Nazaré
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Prof. Dr. Piotr Zielenkiewicz
Rui Moreira
Fernanda Borges
Anna-Lena Gustavsson
Erik Chorell