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The pourpose of this work, based on my PhD thesis, was to develop a prototype of a homogeneous high throughput screening (HTS) for the identification of novel integrin antagonists. HTS is an extremely current topic in pharmacological research in order to withstand the necessity to provide a biological identity, in a reasonable time, to the ever increasing myriad of novel compounds obtained by Combinatorial Chemistry. I hope that the manuscript hereby presented could be a useful tool to other scientists who approach HTS for the first time and would like to develop their own original method.