Hit validation is needed to determine whether a molecule identified in a screen or assay will eventually lead to a drug. Therefore secondary assays generating data about potency, selectivity and functional biochemical activity have to be performed. Lead optimisation is an iterative process involving computer-assisted molecular modelling, chemical synthesis of new compounds and functional assays.
BIA technology has an enormous capability for the rapid confirmation of hits from high throughput screens by a comprehensive kinetic characterisation of potential lead compounds. Informations about affinities, rates of association and dissociation in complex formation and binding stoichiometries are valuable for a ranking and optimisation of lead compounds. Even compounds binding with low affinity or transient kinetics, often found in early phases of drug development, can accurately be identified.
BIA technology provides detailed information how structural changes affect association and dissociation rates and allow a quantitative structural and functional activity relationship analysis (QSAR) in drug discovery processing.
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