Novel advances in assay development and screeningtechnologies to improve lead discovery and increasecorrelation to in vivo and clinical results

Stem Cell AssaysRoberto Iacone, F. Hoffmann-La Roche

3D Cell CulturesPatrick Steigemann, Bayer Pharma AG

Target De-ConvolutionNeil Carragher, University of Edinburgh

Primary CellsDarren Cawkill, Neusentis (A Pfizer Research Unit)

Phenotypic ProfilingMohanraj Dhanabal, EMD Serono

Pioneering Technologies for Cell AnalysisAnker Jon Hansen, Novo Nordisk A/S

Converting Data into KnowledgePeter Horvath, ETH Zurich

Connecting Industry, Academia andTechnology Providers to IncreasePrediction in Lead Identification

To register: +44 (0) 20 7017 7481 registrations@informa-ls.com

Cell Based Assays,Phenotypic Screeningand PioneeringTechnologies

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18-19 March 2014 Hotel Palace Berlin, Berlin, Germany

CONFERENCE

Event Partners:

Pharma / BiopharmPrices from £799*

Academic Prices- Flat Rate £499*

60+ Speakers - 10+ Hours of Networking

• Designing More Physiologically Relevant Cellular Assays forComplex Pathways – 8 industry cases studies on theimplementation of more physiologically relevant assays in HTSprogrammes to improve the prediction of in vivo behaviour

• Target De-Convolution – Uncover the application of noveltechnologies to de-convolute the target and mechanism ofaction from phenotypic screening results

• Obtaining Sources of Physiologically Relevant Cells in HighVolumes – Merck KGaA and Roche discuss strategies forobtaining reliable sources of physiologically relevant cells inhigh volume in our strategic panel discussion

• Converting Data into Knowledge: Extracting Meaning fromComplex Data – Establish best practices and tools to analysemulti-parameter readouts and validating the results ofadvanced cellular screens

• Part of Drug Discovery Innovations – 1 Exhibition • 3 Conference Streams • 1 Location

Conference Highlights for 2014

part of

CONFERENCE

CONFERENCE

CONFERENCE

Cell Based Assay Developments, PhenotypicScreening and Pioneering Technologies

Advances in Target Based Drug Discovery- GPCRsand Epigenetics

Novel Approaches to Drug Design and LeadOptimisation

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Agenda at a GlancePRE-CONFERENCE SYMPOSIUMS: 17 March 2014

DAY ONE: 18 March 2014

Symposium APractical Strategies for Developing 3D Cell Culture Assays and 3DTissue Models for Use in Drug Discovery

Symposium BExploring New Chemical Space and Unlocking NonDruggable Targets

POST-CONFERENCE SYMPOSIUMS: 20 March 2014Symposium CNatural Products- Application and Development in Drug Discovery

Symposium D

Allosteric Modulators in Drug Discovery

Evening Seminar, Discussion and Dinner: 18 March 2014

Establishing and Evaluating the Success of Collaboration Models and Open Innovation in Accelerating Early Stage Drug Discovery

Designing More Physiologically RelevantCellular Assays for Complex Pathways andImplementation in HTS Programmes

Morning Coffee and Exhibition Viewing

Networking Lunch and Exhibition Viewing

Afternoon Tea and Speed Partnering

End of Day One: Networking Drinks Reception

Designing More Physiologically RelevantCellular Assays for Complex Pathways andImplementation in HTS Programmes

Designing More Physiologically RelevantCellular Assays for Complex Pathways andImplementation in HTS Programmes

Fragment Based Screening

Obtaining Sources of PhysiologicallyRelevant Cells in High Volume

Converting Data Into Knowledge:Extracting Meaning from Complex Data

Novel Concepts in Lead Optimisation and Drug Design

Cell Based Assays, Phenotypic Screening andPioneering Technologies

Advances in Target Based Drug Discovery – GPCRs and Epigenetics

Novel Approaches to Drug Design and Lead

Optimisation

DAY TWO: 19 March 2014

Target De-Convolution: De-Convoluting theTarget and Mechanism of Action fromPhenotypic Screening Results

Morning Coffee and Exhibition Viewing

Networking Lunch and Exhibition Viewing

Afternoon Tea and Poster Competition

End of Day Two

Increasing Throughput and Improving CellAnalysis Using Flow Cytometry

Cell Based Assay Developments andPioneering Technologies to Enhance LeadIdentification, Cell Analysis and Validation

Cell Based Assay Developments andPioneering Technologies to Enhance LeadIdentification, Cell Analysis and Validation

Employing New Techniques to UnlockClassical / Challenging Membrane Targetsand Modulating Protein-Protein Interactions

Translating the Results from PhenotypicScreens into Drug Products

Techniques to Improve In Vitro TargetValidation

Cell Based Assays, Phenotypic Screening andPioneering Technologies

Advances in Target Based Drug Discovery – GPCRs and Epigenetics

Novel Approaches to Drug Design and Lead

Optimisation

Drug Discovery Innovations Key Logos:

KeynotePresentation

Interactive RoundtableDiscussion

StrategicDiscussion Panel

CollaborativeProject

Case Study

KEYFor attendees with a particular interest in the followingareas please follow the highlighted streams belowRED: GPCRs ORANGE: Epigenetics

Evaluating and Selecting Targets for DrugDiscovery

Understanding the Function andMechanism of Action of Targets

Impact of Biased Signalling and Signalling Pathways on Drug Discovery

Impact of Biased Signalling and SignallingPathways on Drug Discovery

Advancing Drug Discovery UsingBiochemical and Structural Data

Advancing Drug Discovery UsingBiochemical and Structural Data

Application of Novel ScreeningTechnologies and Assay Development for Target Classes

Application of Novel ScreeningTechnologies and Assay Development for Target Classes

Employing New Techniques to UnlockClassical / Challenging Membrane Targetsand Modulating Protein-Protein Interactions

Drug Discovery Case Histories: RecentHighlights in Discovery and Developmentof Novel Drug Products

Understanding and Utilising ReceptorBinding Kinetics in Drug Design

Applying the Knowledge of EpigeneticPathways and Mechanisms of Action intoEffective Drugs

3

DAY ONE: 18 March 2014

Cell Based Assays, Phenotypic Screening and Pioneering Technologies

07:50 Registration

08:20 Chairperson’s Opening Remarks and Welcome Address

DESIGNING MORE PHYSIOLOGICALLY RELEVANTCELLULAR ASSAYS FOR COMPLEX PATHWAYS AND

IMPLEMENTATION IN HTS PROGRAMMES

08:25 Development of Cell-Based Assays for Pain Drug DiscoveryUsing Native Sensory Neurons Native cell types with relevance to pain drug discovery are being used byNeusentis to develop assays with improved physiological relevance overtraditional approaches. Progress towards high-throughput compatible assaysusing both primary rat neuronal cultures and human stem cell derived sensoryneurons will be discussed; along with some examples of applying these cellsfor phenotypic screening.

Darren Cawkill, Associate Research Fellow, Neusentis (A PfizerResearch Unit), UK

09:00 Biological Variation in Advanced Cell Based Assays -Moving from Unwanted to Highly Desired Moving from a reductionist and target-based drug discovery process to aphenotypic and disease-relevant strategy adds new pressure on cell assayperformance. The use of primary cells and even patient-derived material requirehighly developed and robust assays. With a higher level of integrity assays canbe used to assess, not only compounds’ effect on an in vitro function, but alsoon different donors’ responsiveness to a specific mode-of-action. By reducingtechnical assay variation, well-developed phenotypic assays have the potential to fill the gap between early drug discovery and clinical evaluations.

Niclas Nilsson, Head of Section, LEO Pharma, Denmark

09:35 Phenotypic Profiling in a Physiologically Relevant Cell-Based Assay System Using two different primary cell systems we have developed a screening platformfor rapid and reliable quantification of three dimensional vessel formation anddifferentiation of progenitor stem cells towards oligodendritic cells lineage. The assay platform was miniaturised onto a 384 well format to facilitate screeningprocess. We have performed a live cell high content imaging in an automatedhigh throughput manner for screening subsets of focused chemical library.

Mohanraj Dhanabal, Group Leader, Dept of Molecular Pharmacology,SMP, EMD Serono R & D Institute Inc. USA

10:10 The Power of Isogenic Cell Lines as Applied to siRNA andCompound ScreeningHorizon provides definitive and controlled preclinical model systems throughthe use of isogenic cell lines, where the genetic modification of interest canbe directly compared to its matched normal cell. The use of panels of theseisogenic cell lines allows molecularly-defined cellular models to besystematically profiled, thereby providing a powerful tool for theinvestigation of sensitivity and resistance to cancer therapeutics. Morerecently, Horizon has coupled our isogenic cell line library with ourunderstanding of cancer biology and the tumour microenvironment, alongwith siRNA libraries and automation systems to be able to offer a range ofscreening approaches and assay conditions suitable to meet therequirements of almost any project. This talk will cover the scientific value ofthis approach and the value already being realised through client cases.Kam Dhaliwal, VP Sales, Horizon Discovery, UK

10:45 Morning Coffee and Exhibition / Poster Viewing Time

11:15 iPSCs Derived Cellular Models to Investigate Type 2Diabetes Cardiovascular ComplicationsThe development of new medicines for Diabetes Type 2 complications has provento be challenging due to the use of cellular models which recapitulate somesubsets of the specific features of the human disease. Herewith, we describe howthe advent of the patient-specific iPSC technology in combination with the in vitromimicking of the “diabetic microenvironment stressors” allows the study ofsignalling pathways and response to selective drugs in iPSC derivedcardiomyocytes for lead identification in diabetic cardiomyopathies indications.

Roberto Iacone, Head Stem Cells Group, Cardiovascular andMetabolism Discovery, Roche, Germany

11:50 Adult Lgr5 Stem Cells: A Tool for Drug DevelopmentWe identified LGR5 as a unique marker of intestinal stem cells. A novelculture method uncovered the potential of LGR5 stem cells to proliferate asever-expanding organoids in 3D in vitro culture. This culture technology notonly allows the expansion of intestinal LGR5 stem cells but also stem cells ofother healthy and diseased cells of organs such as stomach, liver, pancreas,and prostate. Therefore organoid technology has open new avenues to buildbetter predictive models for drug development that are patient specific.

Robert Vries, Stichting Hubrecht Organoid Technology (HUB), TheNetherlands

12:25 Spotlight PresentationSpotlight presentations are hosted by leading companies within the cellbased assays field. These sessions offer an opportunity to learn about thelatest developments and technologies within industry. For more informationabout hosting a spotlight session please contact: Linda Cole, Tel: +44 (0)20 7017 6631, Email: linda.cole@informa.com

13:00 Lunch and Exhibition / Poster Viewing Time

14:15 High Content Screen and 3D Cell Culture Assays UsingChondrocytesEmploying primary cells for screening can efficiently circumvent this shortageand we performed a high content screen on ~ 600 000 compounds using onebatch of primary pig chondrocytes. In this phenotypic setup, we weresearching for compounds inducing cell proliferation, differentiated chondrocytephenotype and expression of Sox9. In addition, to foster more relevant in vitroscreening for more advanced project compounds; we established a 3Dhanging drop culture to evaluate different chondrocyte cell lines with respectto secretion of cytokines as well as expression of a few relevant genes.

Christa Burger, Principle Scientist, Molecular Pharmacology, MerckKGaA, Germany

14:50 Trends in Cell Based Assays: Stem Cells, 3D & Live ContentImagingThis presentation will highlight the convergence of developments in humanstem cell technology, micro-tissues and live cell kinetic imagingmeasurements (‘Live Content’) in delivering more relevant, informative yettechnically practical assay solutions for drug discovery. By way ofexemplification, validation data from a range of 96/384-well live contentassays including neurite outgrowth dynamics in hIPSC-derived neurones,vascular tube formation and stabilisation in mesenchymal stem cell co-cultures, and growth and shrinkage in 3D-tumour spheroids will be shared.

Derek Trezise, Director & Site Head, Essen Bioscience Ltd, UK

15:25 Afternoon Tea and Speed Partnering

OBTAINING SOURCES OF PHYSIOLOGICALLYRELEVANT CELLS IN HIGH VOLUMES

16:05 Strategic Panel DiscussionOvercoming the Challenges in the Availability of PhysiologicallyRelevant Cell Samples and Cell Stability• Strategies for obtaining reliable sources of physiologically relevant cells• Defining physiological relevance: Origin, morphology, functionality• Timeframes for use of physiological cell samples• Approaches for inducing and stabilising physiologically relevant cells overlonger time periods to improve cell stability

Panellists Include: Christa Burger, Principle Scientist, MolecularPharmacology, Merck KGaA, GermanyRoberto Iacone, Head Stem Cells Group, Cardiovascular andMetabolism Discovery, Roche, Germany

CONVERTING DATA INTO KNOWLEDGE:EXTRACTING MEANING FROM COMPLEX DATA

16:40 Multi-Parametric Regression and Active Learning Methodsfor Image-Based ScreeningIn this talk I will give an overview of the computational steps in the analysis ofa single cell-based high-content screen. First, I present image analysis andfeature extraction methods. Then, I discuss the Advanced Cell Classifier(ACC) a software tool capable of identifying cellular phenotypes based onfeatures extracted from the image. For cases where discrete cell-baseddecisions are not suitable, we propose a method to use regression to analysecontinuous phenotypes. Using the ACC program, it is possible to identifydiscrete and continuous cell types parallel. Finally, active learning methodswill be discussed, to improve the speed and accuracy of machine learning.

Peter Horvath, Group Leader, Hungarian Academia of Sciences,Biological Research Centre Senior Scientist, ETH Zurich, Switzerland

17:15 Interactive Round Table DiscussionDesigning More Physiologically Relevant Cellular AssaysTable One: Primary Cell AssaysTable Two: Stem Cell AssaysTable Three: 3D Assays

17:50 End of Day One followed by Drinks Reception in theExhibition Hall

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DAY TWO: 19 March 2014

Cell Based Assays, Phenotypic Screening and Pioneering Technologies

08:55 Chairperson’s Opening Remarks

TRANSLATING COMPLEX PATHWAYS ANDFUNCTIONS INTO SIMPLE CELL BASED ASSAYS

FOR PHENOTYPIC SCREENING

09:00 Application of High Content Imaging and Stem Cells toPhenotypic Drug DiscoveryFor further details of this presentation please refer to the event website atwww.informa-ls.com/ddi

Samantha Peel, Senior Research Scientist, AstraZeneca R&D, UK

TARGET DE-CONVOLUTION: DE-CONVOLUTINGTHE TARGET AND MECHANISM OF ACTION FROM

PHENOTYPIC SCREENING RESULTS

09:35 De-Convoluting the Target and Mechanism of Action fromPhenotypic Screening ResultsPhenotypic screenings is a powerful tool to identify active compounds, butthe identification of their mechanism of action is still a bottleneck. I willdiscuss our approach of multi-parametric phenotypic profiling of compounds,and the methodology to search for similar profiles from a reference geneticscreening, in order to identify mechanism of action of the compounds.

Rico Barsacchi, Scientist, TDS, Max Planck Institute of Molecular CellBiology and Genetics, Germany

10:10 Advancing Drug Mechanism-of-Action Studies throughCombined Imaging and Pathway Profiling Technologies withinDisease Relevant Preclinical Models Limited understanding of drug mechanism-of-action and pharmacologicalresistance contributes to poor efficacy and attrition at later stages of drugdiscovery and development. We demonstrate how multi-parametric highcontent imaging and Reverse Phase Protein Microarray (RPPA) technologiescan combine to enable a robust and unbiased approach to profilingcompound mechanism-of-action and optimising efficacy within complex invitro and in vivo settings.

Neil Carragher, Principal Investigator, Edinburgh Cancer Research UKCentre, Institute of Genetics and Molecular Medicine, University ofEdinburgh, UK

10:45 Morning Coffee and Exhibition / Poster Viewing Time

11:15 Spotlight PresentationSpotlight presentations are hosted by leading companies within the cellbased assays field. These sessions offer an opportunity to learn about thelatest developments and technologies within industry. For more informationabout hosting a spotlight session please contact:Linda Cole, Tel: +44 (0)20 7017 6631, Email: linda.cole@informa.com

INCREASING THROUGHPUT AND IMPROVING CELL ANALYSIS USING FLOW CYTOMETRY

11:50 Increasing Efficiency and Automation of Flow CytometryFor further details of this presentation please refer to the event website atwww.informa-ls.com/ddi

Rob Jepras, Senior Investigator, Biological Sciences, RD PlatformTechnology & Science, GSK, UK

12:25 Application of Flow Cytometry in Drug DiscoveryFor further information on this talk please visit the event websitewww.informa-ls.com/ddi

Frederik Stevenaert, Senior Scientist, Janssen PharmaceuticalCompanies, Belgium

13:00 Lunch and Exhibition / Poster Viewing Time

CELL BASED ASSAY DEVELOPMENTS ANDPIONEERING TECHNOLOGIES TO ENHANCE LEADIDENTIFICATION, CELL ANALYSIS AND VALIDATION

14:15 Light Sheet-Based Fluorescence Microscopy and Three-Dimensional Cell Cultures Advance Cancer Diagnosis and Drug DevelopmentBenefits of tumor spheroids in novel autophagy flux and apoptosis assays areexplained and an outlook on induced pluripotent stem (iPS) cell-basedspheroid models in drug toxicity testing is provided. Light sheet-basedfluorescence microscopy (LSFM) is the state of the art technology forobservations of cellular and sub-cellular dynamic processes in three-dimensions over time with high spatio-temporal resolution and high-throughput applications.

Nariman Ansari, Scientist, Physical Biology, Buchmann Institute forMolecular Life Sciences (BMLS, CEF-MC), Goethe UniversitätFrankfurt ,Germany

14:50 Impedance Sensing as a Label-Free TechnologyImmune cells and endothelial cells are important for inflammation and formany diseases. The talk shows how a label-free technique like impedancemeasurement can be used to measure cell adhesion, cell activation and celldeath. Especially immune cells exhibit rapid changes in adhesive propertiesthat cannot be measured by conventional methods. Likewise onlinedetermination of barrier function of endothelial cells is convenient measuredby impedance.

Anker Jon Hansen, Scientific Director, Immunobiology, Novo NordiskA/S, Denmark

15:25 Afternoon Tea and Exhibition / Poster Competition

16:05 Increasing Efficiency, Lead Discovery and Validation: NovelHigher Throughput Technologies for in vitro AssaysFor further details of this presentation please refer to the event website atwww.informa-ls.com/ddi

Andreas Mühlemann, Lab Head, CNS Biology,Actelion Pharmaceuticals Ltd, Switzerland

TECHNIQUES FOR IMPROVING IN VITRO TARGET VALIDATION

16:40 New Methods for Improving In Vitro Target Validation• Evaluating novel technologies for improving target validation at the cellular level

• Increasing translation to in vivo• Methodologies for validating receptor responses and activity• New techniques for biochemical and cellular knock out models• Methods for target validation for large scale siRNA/shRNA screens• Application of genome editing tools to improve in vitro target validation

Panellists made up from a selection of speakers throughout the event

17:15 Closing Remarks from the Chair and End of Conference

Very interesting array of examples of the use of phenotypic, cell based assays and

the challenges that were overcomeChief Scientific Officer, Trophos, 2013

Warm atmosphere with useful and motivating discussions

Project Promoter & Leader, Associate Director, Drug DiscoveryDept., Actelion Pharmaceuticals Ltd, Switzerland, 2013

Media Partners:

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Registration: 10:00. Start: 10:30. End 16:30. • Lunch, Morning and Afternoon Refreshments will be included.

PRE-CONFERENCE SYMPOSIUMS: 17 March 2014

Registration: 18:35. Start: 18:45. End 20:30 • A Networking Dinner will follow for all seminar attendees.

EVENING SEMINAR, DISCUSSION AND DINNER: 18 March 2014

SYMPOSIUM A: Practical Strategies for Developing 3D Cell CultureAssays and 3D Tissue Models for Use in Drug Discovery

IntroductionFor drug discovery, cell-based assays are getting increasingly complex in order tomimic more realistic biological processes and their diversifications in diseases.Multi-cellular co-cultures embedded in 3D matrices have been explored to moreclosely approximate the physiology of the human microenvironment. This multi-speaker symposium will focus on overcoming the practical challenges of designingand screening with complex 3D cell culture assays in high throughput and highcontent screening platforms. Culture technologies and techniques for mimickingthe culture in a well will be discussed as will the application of these technologiesin drug discovery. The design of 3D tissue modelling systems will also be discussedas strategies for improving target identification and validation.

Take home messagesHow to mimic the disease state feasibly?- Setting up effective functional screens using 3D cell cultures - Assay design: How to adapt and develop 3D assays for HTS and HCS

Evaluation of 3D matrix materials and reagents for establishing 3D cell cultures - Dealing with variations in matrix materials- Protocols for handing 3D matrix media in automated systems- Costs

Transitioning from 2D to 3D assays- Integrating 3D cultures with traditional screening platforms

Developing 3D tissue cultures - Strategies to grow 3D tumour-like spheroids and tissues in screening well

Application of 3D assays to identify the target from phenotypic screening

Benefits of 3D assays in drug discovery- Comparison between 2D and 3D assays and transfer to in vivo development- Are the results from 3D screens better than 2D results for in vitro screening?

Case studies on the application of 3D cell culture assays drug discovery

Symposium Leaders:Patrick Steigemann, Scientist, Bayer Pharma AG, GermanyLaure Bouchez, Research Investigator II, Novartis, SwitzerlandAnthony Davies, Director, Irish National Center for High-ContentScreening and Analysis (INCHA), IrelandMike Atkinson, Director of Institute of Radiation Biology, HelmholtzZentrum München and Chair of Radiation Biology, Technical UniversityMunich, GermanyFor more information of this symposium please see the event websitewww.informa-ls.com/ddi

SYMPOSIUM B: Exploring New Chemical Space and Unlocking Non-Druggable Targets

IntroductionThe ability to explore new chemical space is essential to establish new ways toprevent and treat disease and advance drug discovery. With the advancement innew technologies the potential to access previously non-druggable targets hasbeen made possible. This multi-speaker symposium will focus on overcoming thepractical challenges of exploring new chemical space, discuss the best ways tosearch for new small molecules and provide an overview on the development oftools and technologies to unlock previously non-druggable targets.

Take home messagesExpanding the druggable genome

Efficient sampling of chemical space

Tools and technologies to identify novel target space

Technologies to explore new chemical space and unlock and address difficult targets

Use of historical biological assay data to efficiently sample bioactive chemical space

New chemistries for non-drugable targets

Chemical probes for target validation and pathway analysis

Lead identification techniques for difficult to address targets

Drug design strategies for less defined binding pockets

Symposium Leaders:Anne Mai Wassermann, Presidential Postdoctoral Fellow, NovartisInstitutes for Biomedical Research, USAFor more information of this symposium please see the event websitewww.informa-ls.com/ddi

Establishing and Evaluating the Success of Collaboration Models and Open Innovation in Accelerating Early Stage Drug Discovery

IntroductionThis highly interactive evening seminar will address and provide real-life practicalexperience on the implementation of different collaboration models to advanceearly stage drug discovery. Perspectives from large / small pharma and academiawill be presented in short 20 minute case study presentations with a key emphasisbeing placed on:How companies are tackling the major bottlenecks observedEvaluating the success of collaboration results from each approachLessons learnt from experiences

Case study presentations will be followed by an interactive discussion with theaudience allowing the opportunity to share experiences of the impact ofcollaboration models on end results, strategies for translating drug discoveryexternalised projects to the next level and evaluating the impact and managementof an ever changing R&D landscape on present and future collaborations.

Take home messagesEstablishing effective models for collaborations in early stage drug discovery

Which models are best suited to different stages of drug discovery?

Applicability of model to run alongside other models

Minimising IP risks in collaborative research

Can models be used to validate new targets and drug candidates?

Do these models deliver?

Open innovation: Are new targets and compounds being identified usingthese methods?

EU-OPENSCREEN as a novel collaboration model

Management: Establishing effective collaborations between pharma and academia- How to best work together to both benefit from collaboration- Meeting expectations and translating research into commercial products- External and internal alignment for successful collaborations

Lessons learnt: Evaluating what’s working and what’s not working

Adding value to pipelines: Translating project results and ideas into products- How and what will be taken forward into future alliances and translating into future medicines

Seminar Leaders:Ulrich Betz, Director Department Head Innovation & EntrepreneurshipIncubator, Global Business Development & Strategy,Merck Serono,GermanyStefan Jaroch, Head, External Innovation Technologies, Bayer, GermanyRonald Frank, Coordinator of EU-OPENSCREEN, Leibniz-Institut fürMolekulare Pharmakologie (FMP), GermanyBert Klebl, CEO & CSO, Lead Discovery Center GmbH, Germany

Free to Attend with a 4 Day Pass

A state of the art overview with practical hints and discussion on the pros and cons of technologies and modelsUniversity of Santiago de Compostela,

Symposium Attendee 2013

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Registration: 08:30. Start: 09:00. End 15:00. • Lunch, Morning and Afternoon Refreshments will be included.

POST-CONFERENCE SYMPOSIUMS: 20 March 2014

SYMPOSIUM C: Natural Products – Application and Development inDrug Discovery

IntroductionOver the years, natural products have proved be to an important source of leadcompounds and therapeutic agents for drug discovery; however thedevelopment of these leads into medicines has previously been hampered by thecomplex molecular architecture of natural products which impacts chemicaltractability. Recent technological advancements have allowed the bioactive ofnatural products to be evaluated successfully re-establishing natural products asa major easy-to-use source in drug discovery programmes. This multi-speakersymposium will focus on the identification and development of natural productleads into drug discovery products.

Take home messagesNatural product screening, target identification and assay development- Application of natural product libraries to identify new targets and chemicalcompounds for drug discovery- Overcoming the challenges in selecting new drugs from natural productlibraries- Combining natural product collections with advanced cell based assays to identify new leads- Novel technologies in the discovery of natural products

Understanding biological function with natural products- De-convoluting the target mechanism of action from natural product library screens- Probing biology with natural product fragments - Technologies to associate biological function with results- Translating chemical biology into human biology

Natural products and synthetic biology- How can recent advances in synthetic biology help drive natural productresearch to facilitate drug discovery?

Natural product lead optimisation and drug product development- Understanding chemistries and lead optimisation of natural products- Case studies on recent highlights in the discovery and development ofnatural drug products

Symposium Leaders:Tim Schuhmann, Investigator III, Novartis Pharma AG, SwitzerlandKarl Gademann, Department of Chemistry, University of Basel,SwitzerlandAndrea Alimonti, ERC Investigator, Head Molecular Oncology,Institute of Oncology Research (IOR), SwitzerlandArmin Bauer, Head of Medicinal Chemistry II, R&D LGCR / Chemistry FF,Sanofi-Aventis Deutschland GmbH, GermanyFor more information of this symposium please see the event websitewww.informa-ls.com/ddi

SYMPOSIUM D: Allosteric Modulators in Drug Discovery

IntroductionFor a receptor to illicit a response, the ligand does not have to bind to the ligandbinding site. By certain factors binding to other sites on the receptor, this cancause a change in the downstream signalling of the receptor. By identifying theseallosteric ligands it is possible to exploit them as a potential leads in drugdiscovery. However the identification and characterisation of allosteric modulatorsusing standard assays and the translation into the clinic has proven challenging indrug discovery. This multi-speaker symposium will focus on novel tools to identify,validate and understand allosteric modulators and present latest developments ontheir translation into later stage drug discovery.

Take home messagesTools to identify and understand allosterism- Technologies and methodologies to identify, characterise allosteric modulators and understand allosterism- Characterising mechanisms of action and functionality of allostericmodulators- Adapting screening strategies to novel GPCR modulation paradigms

Allosteric modulators lead optimisation and drug product development- Lead optimisation of allosteric modulators- Understanding chemistries- Novel approaches for allosteric modulators- Case studies on recent highlights in the discovery and development ofallosteric drug products

Overcoming the challenges in translating allosteric modulators into laterstage drug development

Proof of concept, in vivo effects of allosteric modulators

Translating allosteric modulators into clinical trials

Targeting allosteric modulators in drug discovery

Translating knowledge from allosteric modulators for GPCRs to other target classes

Symposium Leaders:Sylvain Celanire, PhD, CNS R&D Professional, former Associate DirectorMedicinal Chemistry, Addex Therapeutics, SwitzerlandStephan Schann, Head, Research, Domain Therapeutics SA, FranceFor more information of this symposium please see the event websitewww.informa-ls.com/ddi

Best Paper Award: Sponsored and judged by

In recognition of the significant educational impact and value papers provide our attendees, the publishers atComputational and Structural Biotechnology Journal have created the 2014 Drug Discovery InnovationsBest Paper Award.

Computational and Structural Biotechnology Journal will be the forum for the publication of selected papersfrom the Drug Discovery Innovations Conference 2014. Participants presenting and attendees at DDI 2014 areencouraged to submit their work as full length manuscripts to Computational and Structural BiotechnologyJournal. CSBJ will devote a special volume comprised of articles from the speakers/oral and poster presentersof the Drug Discovery Innovations Conference 2014.

Among the paper submissions CSBJ will receive, the Editorial team will review and select an article from thefull length manuscripts submitted to CSBJ by the participants/attendees of DDI 2014 for the Best Paper Awardof $500* with the winning paper announced at the conference.

To apply for the CSBJ Best Paper Award please see the event website for full details www.informa-ls.com/ddi

Present a Poster at the Event

• Posters submitted by academics, biopharmaceutical and pharmaceutical organisations will not be charged a fee

• Posters submitted by service providers/vendors are welcome and will be subject to evaluation by the scientificadvisory board. Upon approval a fee of £399 + VAT will apply

Last date for poster submission is Friday 21 February 2014

*See event website www.informa-ls.com/ddi for full terms and conditions for paper submissions for CSBJ Best Paper Award

Present a Poster at the Event or Submit a Paper to Win $500*

Drug Discovery Innovations is doubtless a must-event!

Director and Owner, Atheris Laboratories, 2013

18-19 March 2014 Hotel Palace Berlin, Berlin, Germany

Drug Discovery Innovations 2014 - Sponsorship and Exhibition Opportunities

A clear focus on enabling top scientific and industry leaders to connect and learn inan environment that fostered meaningful interactions. For my money, this is one ofthe best meetings of its kindVP Sales at Horizon Discovery

The meeting was not only perfectly organised, it was also attended by a broadaudience of high level decision makers, most of whom I had not met before.“Drug Discovery Innovations" is a must-attend event!Director and Owner, Atheris Laboratories

VITAL STATISTICS130+ attendees

60+ industry speakers

100+ companies represented

10+ hours of dedicated networking

2013 AUDIENCE ANALYSIS

14%VP & C-Level

27%Senior Scientists& Researchers

SpeedPartnering

DrinksReception

Scientific PosterSession

Exhibition Hall Round TableDiscussions

Joint Exhibitor andDelegate Lunch Sessions

40%Heads & Managers

19%Academia

Attendee Job Title Breakdown

• Assay Development• Chemical Biology• Computational Chemistry• Discovery Chemistry• Drug Design • Drug Discovery• Epigenetics• GPCRs• In-Vitro PharmacologyDepartment

• Lead Identification / Discovery /Generation

• Lead Optimisation• Medicinal Chemistry• Molecular and CellularPharmacology

• Molecular Biology • Oncology• R&D• Screening and CompoundProfiling

• Structure Based Drug Design• Target Identification andValidation

Directors, Managers, Heads of Departments, Team Leaders,Investigators and Principal / Senior / Research Scientists from:

WAYS TO MEET PEOPLE - Utilise our networking and interactive activities to improve your conference experience

1 Exhibition • 3 Conference Streams • 1 Location

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For more information on the opportunities available please contact Linda Cole Email: linda.cole@informa.com Tel: +44 (0)20 7017 6631

WHY JOIN DRUG DISCOVERY INNOVATIONS 2014?Save time and money: Meet all your prospects in one location

3 conference streams delivering real data and facilitating the exchange of knowledge and ideas:

Cell Based Assay Developments, Phenotypic Screening and PioneeringTechnologies

Advances in Target Based Drug Discovery

Novel Approaches to Drug Design and Lead Optimisation

Present your latest scientific developments or launch new technologyproducts on the conference programme to the sectors most importantdecision-makers

Build brand awareness amongst industry’s best through an exhibition standand extensive marketing opportunities that guarantee you achieve high visibility

NEW for 2014: DDI Innovation HubContact us for more information on the flexible packages we can tailor-makefor new clients and smaller organisations

For more information on the opportunities available please contactLinda Cole, Email: linda.cole@informa.com Tel: +44 (0) 20 7017 6631

2014 Event Partners:

INVESTMENT OPTIONS

#DrugDiscovery@DDI2014

NOTE: The VAT rate is subject to change and may differ from the advertised rate.The amount you are charged will be determined when your invoice is raised.

*T&CS DISCOUNT PROMOTION: 1. Only applicable for the 2 main conferencedays and not available on add-on days. 2. Not applicable to supplier/vendorcompanies. Only available for biopharm and pharmaceutical companies.

Informa Life Sciences will verify whether you are a vendor/supplier when yourregistration is processed.

4. SME/Industry start ups only available to biopharm and pharmaceuticalcompanies. 5. Discounts cannot be accumulated.

SUBMIT A POSTER:

FREE for Standard Industry, Academic, Start-Up and SME Delegates

Supplier/Vendor £399 + VAT @ 20%

Pre and Post-Conference Symposiums & Evening SeminarMonday 17 March - Pre- Conference SymposiumsApplication and Practical Strategies for Developing 3DCell Culture Assays and 3D Tissue Models for Use in DrugDiscovery AExploring New Chemical Space and Unlocking NonDruggable Targets B

Tuesday 18 March - Evening Seminar, Discussion and DinnerEstablishing and Evaluating the Success of CollaborationModels and Open Innovation in Accelerating Early StageDrug Discovery S

Thursday 20 March - Post - Conference SymposiumsNatural Products- Application and Development in DrugDiscovery CAllosteric Modulators in Drug Discovery D

To make payment by credit card: to ensure we provide the highest level of security for your credit card details we are unable to accept such payments via email or fax which ensures that these details are never stored on our network. Tomake payment by credit card on-line, please enter your credit card details in our secure payments website that you will use when making your booking via the event website (the event web address is near the top of the booking form).Alternatively call our customer service team on +44 (0) 20 7017 7481.Due to unforeseen circumstances, the programme may change and Informa reserves the right to alter the venue and/or speakers. ©Copyright Informa BV, 2013/2014

CQ2260C

18-19 March 2014Hotel Palace Berlin,Berlin, Germany

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Booking Contact:

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Nature of Company BusinessNo. of employees on your site:

1) 0-49 2) 50-249 3) 250-499 4) 500-999 5) 1000+

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DELEGATE DETAILS – Please photocopy form for multiple bookings!

To assist us with future correspondence, please supply the following details:

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STANDARD INDUSTRY RATES* SUPPLIER/ VENDOR RATES

£799 +19%VAT= £950.81

£998 +19%VAT= £1187.62

£1198 +19%VAT= £1425.62

£1397 +19%VAT= £1662.43

£1399+19%VAT= £1664.81

Book BEFORE Dec 13th 2013

£1799 +19%VAT= £2140.81

£1998 +19%VAT= £2377.62

£2198 +19%VAT= £2615.62

£2397 +19%VAT= £2852.43

£2399+19%VAT= £2854.81

Book BEFORE Dec 13th 2013

£999 +19%VAT= £1188.81

£1198 +19%VAT= £1425.62

£1398 +19%VAT= £1663.62

£1597 +19%VAT= £1900.43

£1599+19%VAT= £1902.81

£300

£300

£300

£300

£500

SAVE

£200

£200

£200

£200

£400

Book BEFORE Feb 14th 2014

£1199 +19%VAT= £1426.81

£1398 +19%VAT= £1663.62

£1598 +19%VAT= £1901.62

£1797 +19%VAT= £2138.43

£1799+19%VAT= £2140.81

Book AFTER Feb 14th 2014

£1899 +19%VAT= £2259.81

£2098 +19%VAT= £2496.62

£2298 +19%VAT= £2734.62

£2497 +19%VAT= £2971.43

£2499+19%VAT= £2973.81

Book AFTER Dec 13th 2013

2 Day Pass: Conference Only

2 Day Pass: Conference + Evening Seminar

3 Day Pass: Conference + Pre or Post Conf Workshop

3 Day Pass: Conference + Pre or Post Conf WorkshopAND Evening Seminar

FULL Pass: Conference + Pre AND Post Conf Workshop+ FREE Evening Seminar

VENUE DETAILS:Hotel Palace Berlin, Budapester Str. 45 10787 Berlin Tel.: +49 30 2502-0 Fax: +49 30 2502-1119 www.palace.de hotel@palace.de

REDUCED RATE ACCOMMODATION: The cost of accommodation is not included in the conference fee.Please visit the event website www.informa-ls.com/ddi, “Accommodation” tab for information on how to bookreduced rate accommodation. Please book early to avoid disappointment.

CONFERENCE DOCUMENTATION: CANNOT ATTEND?For those busy executives who cannot take full advantage of this event, the CD gives you a usefulrecord of the presentations made at the event. The set of speakers papers and/or slides in CD formatfrom the conference is available after the event for £499 + 20% VAT. UK VAT: The VAT rate is subjectto change and may differ from the advertised rate. The amount you are charged will be determinedwhen your invoice is raised. Contact Customer Services on tel: +44 (0) 20 7017 7481, fax +44 (0)20 7017 7823 or e-mail: registrations@informa-ls.com

Terms and ConditionsFEE: This includes all technical sessions, refreshments, lunch and accessto speaker presentations that we have permission to make available.CANCELLATIONS: Cancellations received in writing before and on Monday 3rd March 2014 will be subject to a service charge of £99. The fullconference fees remain payable after Monday 3rd March 2014.Substitutions are welcome at any time. It may be necessary for reasonsbeyond the control of the organiser to alter the content and timing of theprogramme or the identity of the speakers. In the unfortunate event that anevent is cancelled Informa are not liable for any costs incurred by delegatesin connection with their attendance. This contract is subject to English Law.ARE YOU REGISTERED?: You will always receive an acknowledgement ofyour booking. If you do not receive anything please call +44 (0)20 70177481 to make sure we have registered your booking.ANY SPECIAL REQUIREMENTS?: Please inform us if you have anyspecial requirements by calling +44 (0)20 7017 7481

DATA PROTECTION: The personal information shown on this form, and/orprovided by you, will be held on a database and may be shared with othercompanies in the Informa Group in the UK and internationally. If you do not wishyour details to be available to companies in the Informa Group please contactthe Database Manager at Maple House, 149 Tottenham Court Road, London,W1T 7AD, Tel : +44 (0)20 7017 7077, Fax: +44 (0)20 7017 7828 or email:integrity@informa.com. Occasionally your details may be obtained from, ormade available to, external companies who wish to communicate with youoffers related to your business activities. If you do not wish to receive theseoffers, please tick the box .

INCORRECT MAILING: If you are receiving multiple mailings or you would likeus to change any details or remove your name from our database, please contactthe Database Manager at the above address, Tel +44 (0)20 7017 7077, Fax +44(0)20 7017 7828 or email: integrity@informa.com - quoting the referencenumber printed on the mailing label.

Group Bookings:To take advantage of group bookings,

please contact Natalie Crow on +44 (0) 20 33 77 3285 or emailnatalie.crow@informa.com

5 EASY WAYS TO REGISTER+44 (0)20 7017 7481

+44 (0)20 7017 7823

registrations@informa-ls.com

www.informa-ls.com/ddi

The BookingsDepartmentInforma UK LtdPO Box 406Byfleet KT14 6WL

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£100

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£100

£100

£300

Investment options for 2014:Academic Prices -Flat Rate

£499*+ VATSME/industry Start ups - 50%*off the current

price tier + VAT