- Late registration possible until Sunday 29 September 2013
The emergence of Chemical Biology has coincided with increasing numbers of exploratory molecular targets and mechanisms, both therapeutic and non-therapeutic in origin. Screening using miniaturised microtitre plate formats remains the most widely utilised 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 structural based approaches to Hit Identification and Validation, for example x-ray crystallography and NMR spectroscopy.
This course will examine the application of molecular screening in Chemical Biology and Academic focused Drug Discovery.
Aims of event
Participants in the course will be given a solid theoretical and practical introduction into the development of biochemical assays for high throughput screening and the interpretation of results including:
- Molecular screening approaches - what is feasible and learning from past failures.
- Developing assays in different formats for the kinase and protease target classes.
- Detailed kinetic characterisation of enzymes to include Km determination for substrates, IC50 determination for inhibitors, signal stability and assay robustness.
- Screening a small molecule library (including known drugs), data analysis and classifying compounds as Hits, interferers, etc.
- Integrating your research program, design of project critical paths which integrate in-vitro, in-vivo and in-silico elements.
Who Should Apply
Doctoral and pre-doctoral level scientists originating from academic and industrial organisations looking to apply screening based methods to identify chemical tools for use in interrogating their molecular targets and pathways of interest. In addition, the course would well suited to technically focused staff from core facilities or contract research organisations who may currently deliver services based “omics” related platforms and who wish to extend their expertise into chemical biology and small molecule Drug Discovery.