The choice of assay for high throughput screening (HTS) is of strategic importance to the successful identification of chemical entities that can be developed into drugs. During the past decade several technologies have emerged permitting large compound collections to be screened against biologically relevant models in a high throughput fashion. In this review, we summarise the technologies that are available for screening G-protein-coupled receptors (GPCRs) and discuss the issues that impact upon the choice of screening methodology.
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