| 8.30 | |
Registration and coffee
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| 9.00 | |
Chairman's opening remarksFrancois Bertelli, Senior Principal Scientist, Pfizer |
| 9.10 |  |
LEAD DISCOVERY STRATEGIES - ONE SIZE FITS ALL, OR HORSES FOR COURSES?Murray Brown, Manager, Data Interpretation and Business Process, Screening and Compound Profiling, GlaxoSmithKline
- 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
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| 9.50 | |
HOW SUCCESSFUL IS HTS?Niklas Blomberg, Associate Director, Computational Chemistry, AstraZeneca
- 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
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| 10.30 | |
HIT VALIDATION STRATEGIESUlrich Hassiepen, Research Investigator II, Novartis
- Level of the need to reduce false positives
- Impact of assay technologies
- Counter-screening approaches
- Screening in a more bio-relevant form
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| 11.10 | |
Morning coffee
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| 11.40 | |
WHEN A MILLION IS TOO MANY - MAXIMISING HTS RETURNS FROM TRUNCATED RANDOM SCREENING SUBSETSWillem Nissink, Associate Principal Scientist, AstraZeneca
- 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
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| 12.20 | |
HCS AND MULTI-PARAMETER READOUTS: DE-RISKING DRUG DISCOVERY PROGRAMMEKatya Tsaioun, President, Apredica
- 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
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| 13.00 | |
Networking lunch
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| 14.00 | |
IMAGING TECHNIQUES FOR HCS AND HTSAlessandro Esposito, Senior Investigator Scientist, MRC Cancer Cell Unit, Cambridge University
- Unsupervised fluorescence lifetime imaging microscopy
- Identifying molecular or cellular sub-populations
- Practical application and case studies
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| 14.40 | |
ON THE IMPACT OF VIRTUAL SCREENING IN LEAD GENERATIONStefan Schmitt, Team Leader, Computational Chemistry, AstraZeneca
- Integration of virtual screening in the lead discovery process
- Good practice for virtual screening
- Performance of VS in comparison to parallel running HTS approach
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| 15.20 | |
Afternoon tea
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| 15.50 | |
IN-SILICO VERSUS WET SCREENING IN THE CONTEXT OF INTEGRATION STRATEGIESGeorge Keseru, Head of Discovery Chemistry, Gedeon Richter
- 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
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| 16.30 | |
IN SILICO SCREENING IN SUPPORT OF DRUG DISCOVERYJames Campbell, Director, Lead Generation, AstraZeneca
- Defining in silico screening - virtual screening, predictive models and database mining
- Exploiting in silico screening - early drug discovery
- Effective techniques in modern drug discovery
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| 17.10 | |
Chairman’s closing remarks and close of day one
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