Radioligand binding, drug discovery

Radioligand binding assays are a relatively simple but at the same time a very important and efficient tool to study target-ligand interactions. Since they are very videly used in drug discovery and have been described extensively, this section only discusses their fundamental aspects and those aspects that are important for the description of the MS binding assays below . More detailed information can be found in the relevant literature [6, 7, 16-21]. 

Noel, F., D.L. Mendonca-Silva, and L.E. Quintas. 2001. Radioligand binding assays in the drug discovery process potential pitfalls of high-throughput screenings. Arzneimittelforschung 51, 169-173. 

Snyder, building on pioneering work by Roth (129), Cuatrecasas (26), and Rang (130) established radioligand binding as a valuable tool in the drug discovery process in 1973 (131). This led to an explosion in the identification and characterization of new receptors... 

As far as affinity and efficacy of drugs are concerned in their therapeutic activity in humans, the correct measurement of these parameters using well-chosen and reliable methods is highly important for drug discovery. These methods mainly, but not exclusively, concern radioligand-binding techniques and specific functional assays. 

Chapter 28. Drug Discovery at the Molecular Level A Decade of Radioligand Binding In Retrospect... 

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