Efficient Methods for high throughput screening ID

26 Feb 2014

The invention of high throughput screening in the early 1980s was truly revolutionary for the field of medicinal chemistry. It provided a means of finding novel starting points, getting away from natural product and peptidomimetic limitations, but also biasing lead optimisation around single mechanisms.

Today chemical libraries often contain hundreds of thousands or even millions of lead-like compounds. Frequently, a huge number of possible leads are generated, the vast majority of which will lead nowhere, and their investigation represents a considerable expenditure. It is essential to develop smarter and more efficient methods for lead discovery.

On 11 June 2014 influential researchers from across industry and academia will gather to present a series of lectures on the future of hit ID for new medicines. Organised by the Fine Chemicals Group and hosted at the Royal Society of Chemistry's Burlington House, this event will explore a number of opportunities for the future of hit discovery and lead optimisation.

Speakers will include Dr Phil Jones, Director of the European Lead Factory (ELF); a novel initiative funded under the European Innovative Medicines Initiative (IMI) to promote the discovery of novel small molecule candidates for further optimisation by the pharmaceutical industry and academic institutions.

Dr Darren Green, Director of Computational Chemistry at GSK, and Dr Martin Swarbrick, a senior researcher at Cancer Research Technology, will present the contrasting but developing strategies being adopted by mainstream pharmaceuticals and the charity-funded sector. This includes the design of lead-like molecule collections, and how collaborations across the sector can enable key hit discovery activities to be undertaken most cost-effectively.

Proteochemometics is a bioactivity modelling technique which combines data from both the ligand and the protein target to better identify possible hits and this field will be introduced by Dr Andreas Bender from the University of Cambridge. Dr Ola Engkvist from AstraZeneca will present on ways to design molecules to find compound which act in multiple pathways - a trend being recognised as vital in tacking certain diseases such as malaria.

A key parameter in choosing the most effective ligand class to optimise is to choose those compounds with potential to develop the most desirable kinetic profile, not just the highest binding affinity. This topic will be addressed by Dr James Murray from Vernalis. Prof Kevin Burgess from the University of Florida will present on exciting approaches his group have developed for designing molecules to make specific interactions with proteins. The day will conclude with a panel discussion to allow you to engage directly on key issues that have arisen in the course of the presentations.

This event is ideally suited for chemists and screening scientists working on hit discovery and in lead optimisation. Regular breaks and a poster session will provide a great opportunity to discuss your own areas of interest with others in the field. Offers of posters are welcome and students are strongly encouraged to present their own research.

Jack York

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