High-throughput screening is a technology wherein a bioassay is performed with very small quantities of thousands and thousands of compounds. Reactions take place in titer plates containing large numbers of wells. Each well holds a microsample of the compound to test with a particular receptor or enzyme. This operation permits the screening of thousands of compounds in just a few days. The activity and potency of the interaction is also easily measured, and promising leads may be identified quickly.
Nuclear magnetic resonance (NMR) spectrometry and electrospray ionization mass spectrometrya are other techniques used to measure the affinity of a small test molecule (the ligand) bound to a receptor. In varying the collision a John Fenn received the Nobel Prize in 2002 (Rossi DT, Sinz MW. Mass Spectrometry in Drug Discovery).
energy, it is possible to determine the level of energy it takes to dissociate the complex. In this way, it is possible to identify which ligand binds with the receptor with the best pharmacological characteristics.
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