This chapter briefly discusses techniques used to measure drug affinity and effciacy in GPCR systems. The key objective of this exercise is to quantify drug activity in a system independent manner so that predictions of drug activity can be made for therapeutic advantage. It should be noted that GPCRs are unique in the sense that ligand activity can be modified by the proteins with which the receptor interacts. From this viewpoint, the study of GPCRs in recombinant systems of varying makeup should yield valuable information about how receptors translate chemical information into biological activity.
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