A NEW COMBINATION OF PROTECTING GROUPS AND LINKS FOR ENCODED SYNTHETIC LIBRARIES SUITED FOR CONSECUTIVE TESTS ON THE SOLID-PHASE AND IN SOLUTION

A strategy for high-throughput evaluation of combinatorial compound li braries is reported, which circumvents the necessity to test complex m ixtures. The method is based on a new combination of protecting groups , solid-phase linker and rags. The bulk of the library first undergoes a binding assay with the components grafted on beads. A selection of beads carrying strong ligands is stripped from the labelled target and distributed into microvessels. The ligands are cleaved and rinsed int o microeluates. Subsequently, a more detailed characterization with a functional assay in solution determines the best performers, which are identified through the peptidic tag left behind on the corresponding mother bead.