By P. Brescia, G. Barush, P. Banks, B. Larson, B. Binkowski, P. Stecha, N. Cosby
GPCR responses to extracellular signaling events remain a major focus of both academic research and drug discovery efforts as pharmacological targets. Hit to lead applications typically require the pharmacological evaluation of hits from screening campaigns where their dose-response is quantified. This secondary screening usually incorporates a functional assay where the GPCR is expressed in a cell line of relevance. Here we demonstrate the automation of the workfl ow for the assessment of agonist and antagonist activity for the b2-adrenergic receptor endogenously expressed in HEK293 cells using a stably transfected bioluminescent protein that binds cAMP. Data obtained using automated methods were consistent with data generated when using manual methods including data quality and EC50/IC50 precision.