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Application note: GABAA Receptors

11 December 2018 | By

SB Drug Discovery shows the validation of fluorescence and automated electrophysiology assays designed to assess agonists, antagonists and allosteric modulators of these receptors, culminating in a high-throughput electrophysiology assay suited to assessing multiple GABAA receptor subtypes on a single assay plate.

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Webinar highlights: Integrated fragment based approach reveals enzymatic inhibitors with potential therapeutic application

10 December 2018 | By

This webinar, held on 25 October 2018, presented the results from integrated fragment-based approaches for Indoleamine 2,3 dioxygenase 1 (IDO1), an enzyme widely recognised as a drug target for the development of immunotherapeutic small molecules in oncology, unveiling the first ligands able to modulate non-catalytic signalling.

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The role of drug transporters in phenotypic screening

27 November 2018 | By , , ,

The relative failure of molecular target-based drug discovery has led to a return to phenotypic screening. Targets that are intracellular necessitate their drug ligands to pass through plasma membranes, where the protein:lipid ratio is often 3:1 by mass and at least 1:1 by area. The widespread view that most of…

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Application note: NanoBRETTM assay for monitoring of ligand binding to GPCRs in live cells, using the CLARIOstar® and the PHERAstar® FS

17 September 2018 | By

Due to the crucial role of G protein-coupled receptors (GPCRs) in mediating cellular responses to external stimuli, these receptors have been and will remain a prime focus for medical research and the pharmaceutical industry for many years to come. Their importance is especially highlighted by the statistic that 30-50% of…