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P11027
HitHunter™ cAMP Assays  Versatile Assays Validated for Multiple Applications
Presenter Birgit Beyermann-Lopata, DiscoveRx Corp., USA
Additional Authors: Neil Charter, Radhika Kadakia, Hayley Tinker, & Chris Norey

Measurement of cAMP, a ubiquitous second messenger, reports the functional status of a Gs or Gi coupled GPCR. Functional responses help in identification of an agonist or antagonist, and are crucial to many hit-to-lead programs in drug discovery. The HitHunter™ family of cAMP assays offers a simplified, robust, scalable and versatile assay ideal for any HTS campaign. In this study, we demonstrate the applicability of the HitHunter cAMP assays in a diverse range of applications. All of the assays are well suited for measuring agonist and antagonist dose responses in assays such as HitHunter cAMP XS+ and optimized for high-throughput sreening. Endogenous receptor activity requires a high sensitivity approach that is fulfilled by the recently optimized HitHunter cAMP HS+ assay. In addition to measuring GPCR activation in cells, the HitHunter cAMP I kit can be used to analyze receptor activity in membrane preps, which is another application that we will highlight. Finally, the kits can be powerful tools for a number of in vitro applications for additional targets, such as enzymes. We will demonstrate the ability to measure PDE (phosphodiesterase) activity and inhibition in an in vitro format.