SMi’s 4th Annual Conference on High Throughput Screening

23rd to 24th January 2006, Millennium Gloucester Hotel, London Sponsored by: Caliper Life Sciences & Genedata Supported by: HTScreening.net, Combichem.net, Pharmafocus, Pharmafile, Inpharm.com & DrugResearcher.com

Dear Head of High-Throughput Screening,

In recent years pharmaceutical R&D productivity has been experiencing decline despite increased research and development spending.

Research and development or R&D are the activities that are undertaken by companies in order to introduce and innovate new services and products. R&D is the first part of the development process of the company. The goal of R&D is to take the new services and products to the market and add them to the bottom line of the company. A lot of research went into developing Snorilwhich is a safe and effective supplement.

Ten years ago high throughput screening was regarded as the potential saviour of drug discovery, but in reality HTS and uHTS have not lived up to their hype – why is this and what can still be achieved with the use of these assays?

SMi’s 4th Annual Conference, High Throughput Screening – The Application of HTS in current and Future Drug Discovery, will provide attendees with the latest insight into this important application, covering market dynamics, improved technologies and thoughts for the future. Further, the conference will address how HTS-based lead generation can be made to deliver, the benefits of this application and where the industry will be in the next 5 years. Additional key issues to be addressed by leading experts in the industry include, opportunities for in silico screening, the screening of protein-protein interactions and data analysis and mining.

Learn how to deal with critical bottlenecks and other issues reducing the efficiency of the drug discovery process through the use and application of better high throughput screening methods and tools.

A must attend event for those wishing to improve their drug discovery productivity!

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EARLY BIRD BOOKING OFFER
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The early bird registration deadline is 31st October 2005. Please register before this date to receive a reduced rate.

To register simply go to: http://www.smi-online.co.uk/goto/htscreening.asp?emref=T14EP31063506

Offers are also available for group bookings, contact James Holland on
tel: +44 (0)20 7827 6180 or mailto:jholland@smi-online.co.uk
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A unique opportunity to learn from leading industry experts including:

– Dr Jefferson Paslay, Vice President, Screening Science, Wyeth
– Dr Jonathan Mason, Executive Director, Medicinal Informatics, Structure & Design, Pfizer
– Dr Lorenz Mayr, Executive Director, BioChemical Assay Development & Screening, Novartis
– Dr Gregory Kaczorowski, Senior Director, Ion Channel Department, Merck
– Dr David Keeling, Director, Lead Generation Biology, AstraZeneca
– Dr Mary Jo Wildey, Senior Research Fellow; Screening & Compound Logistics Centre Team Lead, Johnson & Johnson
– Dr Alexander Hillisch, Director, Medicinal Chemistry & Head, Computational Chemistry, Bayer Healthcare
– Dr Stephen Clulow, Director, Lead Discovery, Cambridge Antibody Technology
– Dr Dominique Besson, HTS Services Group Leader, Serono

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Benefits of Attending:

– THE APPLICATION OF HTS IN DRUG DISCOVERY TODAY AND TOMORROW: Learn how HTS-based lead generation can be made to deliver and its benefits in lead optimisation and CD delivery. What are the benefits of HTS-based drug discovery? How will HTS progress in the next 5 years?
– OPPORTUNITIES FOR IN SILICO SCREENING: Review the latest techniques taking a close look at ligand and target-based in silico screening
– SCREENING OF PROTEIN-PROTEIN INTERACTIONS: Learn how to interfere with protein-protein interactions, uncover the current challenges and limitations and hear success stories from the Lead Discovery Centre at Novartis
– HOW DOES HTS DELIVER VALUE IN DRUG DISCOVERY? Understand the link between HTS, chemoinformatics and lead generation
– DATA ANALYSIS AND MINING: Hear case examples from top pharmaceutical companies as they discuss preferred methodologies to deliver better leads in the drug discovery process
– INDUSTRY EXPERTS: Network with influential experts from leading pharmaceutical companies and learn from their experiences and expertise

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PLUS A HALF-DAY POST-CONFERENCE EXECUTIVE BRIEFING
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Cell-Based Screening
25th January 2006 (AM), Millennium Gloucester Hotel, London
In association with DiscoverX

Executive Briefing details follow the full conference programme
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For the full conference programme please scroll down

DAY ONE – 23rd January 2006

8.30 Registration & Coffee

9.00 Chairman’s Opening Remarks
Dr Lorenz Mayr, Executive Director, BioChemical Assay Development & Screening, Novartis

THE HIGH THROUGHPUT MARKET
9.10 What has been happening?
– Overview of High Throughput Screening (HTS) and
Its impact on the pharmaceutical industry
– The importance of HTS
– The current opportunities and limitations
– The future of HTS – how will HTS progress over the next 5 years? Dr Mary Jo Wildey, Senior Research Fellow; Screening & Compound Logistics Centre Team Lead, Johnson & Johnson

APPLYING HTS TO DRUG DISCOVERY

THE APPLICATION OF HTS IN DRUG DISCOVERY
9.50 Making HTS deliver
– Keeping HTS efficient
– Tracking success downstream
– The benefits of HTS-based drug discovery
– Future challenges
Dr David Keeling, Director, Lead Generation Biology, AstraZeneca

10.30 Morning Coffee

HTS AS AN INTEGRAL PART OF THE EARLY DRUG DISCOVERY PROCESS
11.00 The business of HTS
– Scaling HTS operations to meet organisational requirements
– Successful partnerships across the organisation for HTS success
– Alignment of HTS priorities with discovery goals
– HTS data deliverables that enable rapid progression of projects
– Investing in HTS related technologies that add value
Dr Jefferson Paslay, Vice President, Screening Science, Wyeth

LEAD GENERATION STRATEGIES

HOW DOES HTS DELIVER VALUE IN LEAD GENERATION?
11.40 The link between HTS, chemoinformatics and lead generation
– Optimising the use of HTS
– Ensuring quality and reproducibility in HTS
– Realising the value and investment of each section
– Developing a high quality hit list
– Setting the proper goals and metrics for HTS
Dr Frank Brown, Senior Research Fellow, Johnson & Johnson

12.20 Networking Lunch

LEARNING FROM OUR MISTAKES
1.50 Delivering starting points for successful lead development
– Corporate compound collections, an historic view
– Leadlike, druglike? Enriching corporate compound files
– Success through compound selection
– HTS and ADME
– How our processes drive physico-chemical properties
Dr Dominique Besson, HTS Services Group Leader, Serono

HIGH THROUGHPUT SCREENING STRATEGIES FOR DISCOVERING ION CHANNEL DRUGS
2.30 Ion channel HTS
– Types of ion channel high throughput screens
– Configuring fluorescence-based assays
– Methods for triggering ion channel activity in HTS
– Automated electrophysiology
Dr Gregory Kaczorowski, Senior Director, Ion Channel Department, Merck

EMERGING SCREENING METHODOLOGIES

3.10 Afternoon Tea

IN SILICO SCREENING
3.40 The emergence of screening methodologies
– Reviewing the techniques – ligand and target-based in silico screening
– Protein structure information as a prerequisite for high throughput docking
– Hit-list processing – combining potency and ADMET aspects
– Problems and success stories
Dr Alexander Hillisch, Director, Medicinal Chemistry & Head, Computational Chemistry, Bayer Healthcare

MICROFLUIDICS
4.20 Global adoption in pharmaceutical screening
– The screening dilemma: more spending, more screening, more technologies have delivered relatively low success
– High throughput or high output? The landscape is changing
– Faster, high fidelity data is the new goal for screeners = less failures in the clinic
– 75% of top pharmaceutical companies have adopted microfluidics to assist the change in screening paradigm – why? Jerome LeClercq, European Marketing Manager, Caliper Life Sciences

5.00 Chairman’s Closing Remarks and Close of Day One

5.10 Networking Drinks Reception Sponsored by DiscoverX

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DAY TWO – 24th January 2006

8.30 Re-registration & Coffee

9.00 Chairman’s Opening Remarks
Dr Stephen Clulow, Director, Lead Discovery, Cambridge Antibody Technology

PROTEIN-PROTEIN INTERACTIONS

9.10 SCREENING OF PROTEIN-PROTEIN INTERACTIONS VIA HIGH CONTENT
BIOCHEMICAL ASSAY TECHNOLOGIES
– Interfering with protein-protein interactions – current challenges/limitations
– Generating new target-specific compound collections: The key requirements
– Impact of novel assay technologies on modern drug discovery with difficult targets
– Ultra-sensitive, multi-mode assay technologies for studying protein-protein interactions
– Success stories on protein-protein interactions from the Novartis Lead Discovery Center (LDC)
– Future directions of miniaturised multi-mode high content biochemical screening Dr Lorenz Mayr, Executive Director, BioChemical Assay Development & Screening, Novartis

9.50 HOMOGENOUS ASSAYS FOR PROTEIN-PROTEIN INTERACTION
– Homogeneous protein-protein assays in lead isolation and optimisation
– Case studies for receptor-ligand and antibody-antigen interactions
– Comparison of different assay technologies
– Optimising assays to get the best hits
– How protein-protein assays influence hit to lead attrition
Dr Stephen Clulow, Director, Lead Discovery, Cambridge Antibody Technology

10.30 Morning Coffee

KINASE INHIBITORS
11.00 From hits to leads
– Kinase focussed library – design and value
– Screening and support of the drug discovery approach
– ADME screening
– The selectivity issue
Dr Doris Hafenbradl, Director, Biochemical Screening, GPC Biotech

A MINIATURISED KINASE PLATFORM
11.40 Schering’s approach
– Challenges and benefits
– Impacts on assay development, HTS processes, data quality and compound profiling Dr Christian Bergsdorf, Research Fellow, Schering

12.20 Networking Lunch

DATA MANAGEMENT

DATA ANALYSIS AND MINING TO FIND THE BEST LEADS
2.00 Experiences from big pharma
– Analysing the data to get more from the assay results
– Using the activity models to drive further library design and synthesis
– Differentiating the compounds and attrition management using biological fingerprints to select candidates to proceed to preclinical and clinical testing
Dr Jonathan Mason, Executive Director, Medicinal Informatics, Structure & Design, Pfizer

EXTRACTING INFORMATION FROM HIGH THROUGHPUT SCREENING DATA
2.40 Considerations for the setup of data management and analysis
processes
– Scientific data as a product: what makes them “good”?
– Converting complex data into useful information: data management and analysis strategies
– Maximising quality: designs, parameters, controls
– Maximising efficiency: automated processing and manual review of large-scale data sets
– Maximising information content: global analysis of potency and high
content HTS data
Stephan Heyse, Project Head, Genedata

NEW TECHNOLOGIES
3.20 A poisoned chalice?
– Possible goals of introducing new technologies in the HTS and early discovery environment
– Quantitative and qualitative benefits
– Identifying the risks and uncertainties
– How can we justify their costs?
– Some practical challenges to prepare for
Dr Andrew Chadwick, Global Analytics & Life Sciences Consulting, PA Consulting Group

4.00 Chairman’s Closing Remarks and Close of Conference

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PLUS A POST-CONFERENCE HALF-DAY EXECUTIVE BRIEFING ======================================================================
Cell-Based Screening
25th January 2006, Millennium Gloucester Hotel, London

In association with: DiscoverX

About the Executive Briefing:
This executive briefing will cover the benefits of new and emerging cell-based screening assays as critical tools in the pharmaceutical and biotechnology industries. In particular, the session will focus upon the use of high content assays in both drug discovery and development, including their application in target identification and validation, lead selection and optimisation, and preclinical studies. Since high content cell-based assays provide richer biological information at the sub-cellular level, they offer significant advantages over traditional HTS. High Content Screening (HCS) promotes efficient discovery of drugs more efficiently, while allowing substandard candidates to ‘fail fast’, saving both time and money.

8.30 Registration & Coffee

9.00 Cell-based screening – advantages and disadvantages
– Understanding the advantages of cell-based screening
– Understanding the disadvantages of the approach
– User experiences – how effective is cell-based screening in generating validated compound leads?
– Is it more useful in primary or in secondary screens?

9.45 Infrastructures needed for cell-based screening
– Automated cell culture
– Information handling
– Data analysis

10.30 Morning Coffee

10.50 High content vs high throughput screening
– High content, low throughput, cell-based assays?
– Emerging techniques for higher throughput imaging systems
– High throughput, low content, cell-based assays?
– Emerging techniques for lower throughput cell-based systems

11.30 Cell pathway screening for key target classes
– GPCRs
– Kinases
– Transcription factors, including nuclear hormone receptors

12.10 Discussion and questions – review of the session

12.30 Close of Executive Briefing

About the briefing leaders:
Richard M. Eglen (Ph.D. Molecular Pharmacology) is the Chief Scientific Officer at DiscoveRx Corp., a venture-backed private company in Fremont, CA. Dr Eglen was Vice President and Director of the Institute of Pharmacology at Syntex and subsequently Vice President of the Centre for Biological Research at Roche Bioscience until 1999. He then joined LJL Biosystems as Senior Vice President for assay development and later joined DiscoveRx Corp in 2000, and is responsible for all R&D activities. He is the author of over 300 publications, several book chapters, and patents, and serves on several journal editorial boards. He is also a member of the Board of Directors for the Society for Biomolecular Screening.

Dr Sanj Kumar joined DiscoveRx in 2001, as Vice President and General Manager of the Europe Region. During this time, his main responsibility has been the introduction of DiscoveRx’s high throughput screening technologies to the European pharmaceutical and biotech market place.

Before DiscoveRx, he worked for Biacore where he was responsible for the European sales and marketing organisation. Prior to joining industry, his academic career has included studying mitochondrial proteins as a post doctoral fellow in Nagoya, Japan; Studying for a PhD in the Institute of Neurology, London; and working as a Protein Chemist in the Institute of Cancer Research, London.

**********************************************************************
EARLY BIRD BOOKING OFFER
**********************************************************************
The early bird registration deadline is 31st October 2005. Please register before this date to receive a reduced rate.

To register simply go to: http://www.smi-online.co.uk/goto/htscreening.asp?emref=T14EP31063506

Offers are also available for group bookings, contact James Holland on
tel: +44 (0)20 7827 6180 or mailto:jholland@smi-online.co.uk
**********************************************************************

Sponsorship and Exhibition opportunities:

SMi Group offers excellent opportunities to profile your company through tailored sponsorship opportunities. For details contact Adrian Johnston on tel: +44 (0)20 7827 6074 or mailto:ajohnston@smi-online.co.uk

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