Assay Method Information

Assay Name:  Adenosine Receptor Activity Assay
Description:  The activity of the present compounds was evaluated using the GloSensor cAMP assay, which is a new non-radioactive method offering a simple approach to monitor GPCR activity through changes in the intracellular cAMP concentration. This assay uses a mutant form of Photinus pyralis luciferase into which a cAMP-binding protein moiety has been inserted. The binding with cAMP triggers a biosensor conformational change that leads to an increase of light output allowing to evaluate the activity of ligands at the receptor under study. Following pre-equilibration with a substrate, cells stably expressing both the receptor of interest and the biosensor can be used to evaluate GPCR function enabling easy kinetic measurements of cAMP accumulation or turnover in living cells. In particular, the binding affinity is expressed in Ki and the antagonistic activity in IC50.
Affinity data for this assay
 

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