We have shown that electrospray MS is a valuable tool in the screening of bio-active compounds, the main advantages being in the area of complex mixture screening. The potential of MS to provide a chemical fingerprint of the bioactive compounds next to binding/inhibition properties is unique and in fact only matched by similar approaches using NMR. Next to the assay formats described in this article, many more formats have been successfully demonstrated in literature. It is worthwhile to mention the detection of intact protein-ligand complexes by ESI-MS or MALDI-TOF MS as alternative to the assay concepts described in this article that mainly rely on reporter molecules or the detection of dissociated ligands.
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