Radioligand displacement assays

Table 6.2 Training set molecules for a1A adrenergic receptor and their affinity measured in a radioligand displacement assay.

A more detailed pharmacoprofiling of DS-96, which included a CEREP profile for off-target receptor binding (radioligand displacement assays), abbreviated... 

Radioligand displacement assays dominate this area, such as in the first MIP-based immunoassay reported by the group of Mosbach. Here, MIPs prepared against theophylline and diazepam, respectively, were shown to display comparable cross-reactivities to antibodies raised against the two drugs, with respect to a range of structural analogs. 

Bran Recongnition Site Affinity K,(uM) Radioligand/Displacer Brain Region Assay Time, Temperature Buffer... 

K The measure of displacing potency of a ligand in radioligand-binding assay under appropriate conditions, equals K[>. It is commonly estimated from the IC50. using the Cheng-PrusofT equation. 

Screens for receptor binders, as we ve seen, have traditionally used radioligand binding displacement assays, and compounds acting via allosteric modulation won t necessarily show up in these. Functional assays like FLIPR, which in recent years have become widespread, are better ways to find them and may explain why more of them are now turning up. 

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