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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
Department of Chemical Biology (CBIO)
Prof. Mark Brönstrup
Dr. Marc Nazaré
Translational Medicinal and Biological Chemistry Laboratory
Prof. Dr. Ana Martínez
Laboratory of Medicinal Chemistry
Prof. Rodolfo Lavilla
Prof. Dr. Piotr Zielenkiewicz
Rui Moreira
Fernanda Borges
Anna-Lena Gustavsson
Erik Chorell