High Throughput Screening

Francois Bertelli, Senior Principal Scientist, Pfizer.

• Challenges for lead discovery
• Different approaches to hit identification in GSK including diversity HTS, fragments and encoded libraries
• Strengths and weaknesses of the different approaches

Murray Brown, Manager, Data Interpretation and Business Process, Screening and Compound Profiling, GlaxoSmithKline.

• Overview of new target prosecutions - comparison with the recent past
• Number of target prosecutions compared with rise in HTS
• Major failings of HTS - potential for overcoming

Niklas Blomberg, Associate Director, Computational Chemistry, AstraZeneca.

• Level of the need to reduce false positives
• Impact of assay technologies
• Counter-screening approaches
• Screening in a more bio-relevant form

Ulrich Hassiepen, Research Investigator II, Novartis.

• Using an incremental HTS-set subsetting design to facilitate managing the cost of screening a >>1M compound collection
• Rationale, implementation, expectations and results
• Use of frequent-hitter information from historical HTS data for annotation of new screen results

Willem Nissink, Associate Principal Scientist, AstraZeneca.

• Technology and its validation - review
• Mechanisms of human toxicity - how what you do not know may hurt you
• Streamlining and reducing the cost of hit-to-lead and lead optimisation campaigns
• Advanced lead profiling - case studies

Katya Tsaioun, President, Apredica.

• Unsupervised fluorescence lifetime imaging microscopy
• Identifying molecular or cellular sub-populations
• Practical application and case studies

Alessandro Esposito, Senior Investigator Scientist, MRC Cancer Cell Unit, Cambridge University.

• Integration of virtual screening in the lead discovery process
• Good practice for virtual screening
• Performance of VS in comparison to parallel running HTS approach

Stefan Schmitt, Team Leader, Computational Chemistry, AstraZeneca.

• Case study involving a kinase associated with Alzheimer's and other neurodegenerative diseases
• HTS and in-silico screening carried out separately for direct comparison of utility
• How should the industry combine HTS and in-silico to optimise lead generation

George Keseru, Head of Discovery Chemistry, Gedeon Richter.

• Defining in silico screening - virtual screening, predictive models and database mining
• Exploiting in silico screening - early drug discovery
• Effective techniques in modern drug discovery

James Campbell, Director, Lead Generation, AstraZeneca.