G-protein Coupled Receptor Modulator High Throughput screening using the PHERAstar FS from BMG LABTECH to Detect Cisbio HTRF® Assays Miniaturized with Echo® Liquid Handling from Labcyte

Despite many years of study, G-protein coupled receptors (GPCR’s) remain an attractive target for drug discovery. In order to maximize high throughput screening efforts many are turning to miniaturization which requires robust assays, reliable liquid handling and sensitive detection. The beta-2 adrenergic GPCR was used as a model to assess the ability to miniaturize competitive binding assays and cAMP production assays which employ Cisbio’s HTRF^® assay technology. Using the Echo^® liquid handler from Labcyte assays which were miniaturized to 2 μl in 1536 well plates could be performed using the PHERAstar resulting in Z’ values of nearly 0.9 for all tests.