Chemical Biology Screening

Screening using miniaturised microplate formats remains the most widely utilized methodology for identifying novel chemical matter capable of modulating target function in a meaningful, biologically relevant manner. The first practical steps are the selection synthesis, management and subsequent screening of molecular libraries, either small molecule of biological in origin.  The second critical area is the selection, development and prosecution of bio-assays for Primary Hit identification, Validation and Profiling.  In the context of Drug Discovery projects, Hits are the further optimised using multiple criteria including structure activity relationships, selectivity, physicochemical properties and liability. Automation is a key enabler to increase productivity, particularly in hit identification and validation.

This course will examine the application of molecular screening in chemical biology and academic focused drug discovery using realistic scenarios. Experimental work will cover the process from Primary assay development, screening against a small molecule library with Hits profiled in a secondary cell based assay. The course presenters are mainly drawn from the Pharmaceutical industry and have many years of experience in Drug Discovery across a range of indications.

Suggested reading: Macarron et al., Nature reviews Drug Discovery, 2011.

By the end of the course, it is expected that attendees should be able to apply this new knowledge to their own research projects and increase their chances of success.