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PAINS management: an open source model to eliminate nuisance compounds

4 December 2018 | By

High-throughput screening (HTS) technologies have enabled the routine testing of millions of compounds towards the identification of novel ‘hit’ molecules for therapeutic targets. Oftentimes in this drug discovery process, however, compounds that show promising activity in primary screens show no activity during subsequent hit qualification or progression efforts.

Application Notes supplement 2018

4 December 2018 | By

Researchers are always looking more effective and efficient ways of making their work more successful. In this supplement, some of our commercial partners share their data, detailing the application of their technology.

Hit-to-Lead In-Depth Focus 2018

4 December 2018 | By

This In-Depth Focus examines our understanding of the comprehensive and complex innate immune system, to develop novel treatments and an open source model to eliminate nuisance compounds

Screening In-Depth Focus 2018

3 December 2018 | By

This In-Depth Focus looks at a high-throughput approach for measuring intracellular ATP levels to access compound-mediated cellular toxicity, the role of drug transporters in phenotypic screening, and how to leverage the power of HTS in the new and rapidly evolving collaborative drug discovery landscape.

Targets In-Depth Focus 2018

3 December 2018 | By

In this supplement: Omics-informed drug target discovery in combating emerging infectious diseases, and self-delivering RNAi: paving the way for a new class of cancer immunotherapies.

Targeting innate immunity to treat disease: potential therapeutic applications

3 December 2018 | By , , ,

Despite being one of the more ancient aspects of immunity, therapeutic modulation of the innate immune system has rarely been attempted. Innate immunity is intrinsically linked to the generation of inflammation – necessary for signalling to the adaptive immune system but often self-perpetuating and over-exaggerated, leading to deleterious effects, including…

Leveraging the power of HTS in the new and rapidly evolving collaborative drug discovery landscape

1 December 2018 | By ,

Over the last five years drug discovery has undergone a rapid evolution from a closed and proprietary endeavour to an open and collaborative process. Large and small pharma now openly collaborate with each other and the wider academic world to leverage their collective depth of knowledge to increase the chances…

A high-throughput approach for measuring intracellular ATP levels to access compound-mediated cellular toxicity

30 November 2018 | By , , ,

Many drugs fail in clinical trials due to toxicity-related issues; therefore, drug-mediated cellular toxicity should be determined at an early stage in the drug discovery value chain. There are many assay systems that can be utilised to measure cellular toxicity. In this article we demonstrate that intracellular ATP concentrations are…

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…