Conference Documentation: High Throughput Screening (2010)
SMI Publishing, Ltd
April 26, 2010 SKU: SMI2770771
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SMi's industry-leading High Throughput Screening conference returns for its sixth year. The theme of this year's conference will be how to lead HTS down an intelligent route towards lead generation.
Taking place in London, UK, this conference will look at a wide range of issues within the HTS arena under several 'topic umbrellas'. The State of the Industry will look at the best of HTS now, outsourcing and hit-to-lead bottlenecks. Focussing HTS will investigate methods to increase the quality of the leads generated. There will be in-depth studies into In-Silico Screening and GPCRs, and finally, a look to the future in New Screening Technologies.
Questions examined during the conference will include: how successful is HTS now? Is outsourcing worthwhile economically? What are the IP issues? Can intelligent research outperform HTS? Does iterative screening hold the key to obtaining high quality leads? How can we redesign the HTS framework? Do we rely on established assays too much? Can virtual screening ever replace HTS as the standard lead generator? How can HTS be used successfully in harnessing the power of GPCRs? What is the potential for biophysical tools to be used in screening?
Attend this event to discover how High Throughput Screening can be made more intelligent, more focussed and more beneficial in drug discovery.
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- DAY1
- 8.30 Registration and coffee
- 9.00 Chairman's opening remarks
- Francois Bertelli, Senior Principal Scientist, Pfizer.
- 9.10 LEAD DISCOVERY STRATEGIES - ONE SIZE FITS ALL, OR HORSES FOR COURSES?
- 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.
- 9.50 HOW SUCCESSFUL IS HTS?
- 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.
- 10.30 HIT VALIDATION STRATEGIES
- 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.
- 11.10 Morning coffee
- 11.40 WHEN A MILLION IS TOO MANY - MAXIMISING HTS RETURNS FROM TRUNCATED RANDOM SCREENING SUBSETS
- 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.
- 12.20 HCS AND MULTI-PARAMETER READOUTS: DE-RISKING DRUG DISCOVERY PROGRAMME
- 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.
- 1.00 Networking lunch
- 2.00 IMAGING TECHNIQUES FOR HCS AND HTS
- 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.
- 2.40 ON THE IMPACT OF VIRTUAL SCREENING IN LEAD GENERATION
- 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.
- 3.20 Afternoon tea
- 3.50 IN-SILICO VERSUS WET SCREENING IN THE CONTEXT OF INTEGRATION STRATEGIES
- 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.
- 4.30 IN SILICO SCREENING IN SUPPORT OF DRUG DISCOVERY
- 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.
- 5.10 Chairman’s closing remarks and close of day one
- DAY 2
- 8.30 Re-registration and coffee
- 9.00 Chairman's opening remarks
- Peter O'Brien, Veterinary Clinical Pathologist, University College Dublin.
- 9.10 COPING WITH PROCESS ERROR WITHIN A HIGH THROUGHPUT SCREENING CAMPAIGN
- The impact of process error on hit rate and compound selection
- Minimising false positives and false negatives using computational methods
- Designing HTS compound triaging strategies in the presence of process error
- Nicola Richmond, Investigator, GlaxoSmithKline.
- 9.50 SCREENING AND PATHWAY BIOLOGY
- Understanding transcriptional regulatory networks and host pathogen interactions
- Developing new methods for mapping of complex biological systems
- Applications in the treatment and diagnosis of immune-related diseases
- Peter Ghazal, Head of Division of Pathway Medicine, University of Edinburgh.
- 10.30 HOW TO OPTIMISE SCREENING ASSAYS FOR ORPHAN OR LIGANDED GPCRs
- Assay development
- Assay validation
- Assay optimization
- Case studies
- Michel Detheux, Director FAST Business Unit, Euroscreen SA.
- 11.10 Morning coffee
- 11.40 MODELLING NANOPARTICLE AND LIGAND INTERACTION IN FLEXIBLE RECEPTOR MODELS
- Screening with biophysical models
- Enrichment rates for flexible receptor models
- Towards flexible backbone simulations and induced fit
- Wolfgang Wenzel, Scientist, Institute of Nanotechnology, Karlsruhe Institute of Technology.
- 12.20 HIGH CONTENT SCREENING: A CELL MORPHOLOGY BASED SCREEN TO IDENTIFY NOVEL REGULATORS OF CELL-CELL JUNCTIONS
- High Content Imaging screen design
- Analysis methods and data storage in High Content Imaging Screens
- Data mining and post-hoc analysis of High Content Imaging Screens
- Ann Wheeler, Advanced Imaging Facility Manager, Queen Mary University Of London.
- 1.00 Networking lunch
- 2.00 MAXIMISING THE IMPACT OF HTS ON THE PFIZER DISCOVERY PORTFOLIO
- Assessment of the impact HTS has made on the recent Pfizer portfolio
- The design of screening subsets to increase the efficiency of primary screening campaigns
- John Mathias, Head of HTS CoE, Pfizer.
- 2.40 APPLICATION OF HIGH CONTENT ANALYSIS (HCA) IN DISCOVERING TOXICOLOGY SCREENING STRATEGIES
- Evidence for effective use of HCA in cytotoxicity assessment of human toxicity potential
- Salient criteria for predictive cytotoxicity models
- Interpretation and application of HCA cytotoxicity data for optimisation and prioritisation
- Translational cytotoxicity biomarkers for application in drug discovery and development
- Strategies for incorporation of HCA into drug discovery safety assessment
- Peter O'Brien, Veterinary Clinical Pathologist, University College Dublin.
- 3.20 Afternoon tea
- 3.50 HTS - DEVELOPING FUTURE SUCCESS FROM PREVIOUS EXPERIENCE
- Working with target classes
- Backing the right technologies
- Introducing the right target with the right assay to the right chemistry
- Peter Greasley, Lead Generation Science & Strategy Manager, AstraZeneca.
- 4.30 THE FUTURE FOR HTS
- Historical benefits of HTS (including assay technologies and target classes)
- HTS under the current climate in the pharma industry
- Future challenges of HTS - what is Pfizer doing?
- Francois Bertelli, Senior Principal Scientist, Pfizer.
- 5.10 Chairman’s closing remarks and close of day two
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