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Advanced techniques and applications of LC-MS in small molecule drug discovery

16 June 2016 | By , , ,

A key process in drug discovery is the ability to identify new drug candidates by screening chemical libraries of small molecules, natural products or extracts against a biological target and selecting lead compounds with desirable therapeutic effects. Medicinal chemistry has the challenging role of not only ensuring that the chemical…

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A picture is worth a thousand endpoints: high-content imaging in drug discovery

12 September 2016 | By , ,

Over the past few years several factors in the drug discovery industry have come together to drive an increased interest and subsequent surge in the use of high-content imaging. These include the high costs of attrition in the clinic due to lack of efficacy; increased hurdles and rising costs to…

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Human iPSC-derived functional cells are revolutionising phenotypic drug discovery and development

4 September 2018 | By , , ,

Effective drug discovery and development relies largely on the availability of predictive pre-clinical model systems; the absence of which has contributed to late-stage drug failures and high expenditures. New industry acceptance of human induced pluripotent stem cell (hiPSC)-derived cardiomyocyte assay systems for regulatory safety pharmacology is now resulting in broad…

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The relevance of homogeneous radiometric assays in modern drug discovery

14 February 2016 | By ,

In the past two decades, several alternative, non-radiometric assay formats have been developed for the high-throughput screening (HTS) of target classes such as protein kinases, which were previously screened using radiometric assays. Radiometric screening (and the expertise to perform such HTS) has thus declined in recent years...

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Phenotypic profiling in drug discovery

5 June 2019 | By , ,

Image-based phenotypic profiling of small molecules has been used for identification and characterisation of small molecules in drug discovery and can provide important insights into their mechanisms of action (MOA). This article discusses the use of phenotypic profiling in drug discovery and how machine-learning algorithms could help improve objectivity, processing…

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High-content imaging: challenges of the 3D world

17 June 2019 | By ,

The potential of three-dimensional cell culture models is now well-recognised by scientists; however, there are still some challenges. Margaritha Mysior and Jeremy Simpson address some of the common challenges of working with spheroids and organoid models – including how they are developed and how to obtain high-resolution, high-content images and…