Contents:

1 Executive Summary 1.1 Introduction 1.2 Commercialization Models —How to Build a Business Here? 2 Technology Trends In The GPCR Space 2.1 Overview of G Protein -Coupled Receptors (GPCRs) 2.1.1 Background and Biology 2.2 Signal Transduction Systems 2.2.1 New Paradigms of GPCR Signaling 2.2.2 Receptor Cross Talk and Dimerization 2.3 RGS Proteins 2.3.1 GPCR Kinases (GRKs) and Desensitization of GPCRs 2.4 GPCRs as Drug Targets 2.4.1 Background of Known GPCRs 2.4.2 Orphan Receptors 2.4.3 Structural Approaches: A Major Hurdle in GPCR Drug Discovery 2.4.4 Compound Diversity: Role in Lead Identification and Optimization 2.4.5 Screening Technologies 2.5 Conclusions 2.6 Select References from the Literature 3 Commercial Opportunity And Legal Aspects Of Commercialization 3.1 Commercial Opportunity in the GPCR Space 3.2 Market Opportunity for Vendors in the GPCR Screening Space 3.3 Interviews with Industry Experts 3.3.1 Alfred Gray, PhD, Euroscreen SA 3.3.2 Jonathan A.Javitch, MD, PhD, Associate Professor of Psychiatry and Pharmacology at Columbia University 3.3.3 Mark Pausch, PhD, Principal Research Scientist at Wyeth-Ayerst Research 3.3.4 Carson R.Loomis, PhD, Vice President of Research, Norak Biosciences 3.4 The Property Landscape for GPCRs and Other Biologics 3.4.1 Intellectual Property Overview 3.4.2 Trademarks and Service Marks: Logos and Brand Names 3.4.3 Copyright: Written and Audiovisual Works 3.4.4 Trade Secrets: A Grab-Bag of Perpetual Secrets 3.5 A Short Patent Prime 3.5.1 Patents: Procedures and Players 3.6 After the Grant: Patent Litigation and Licensing 3.7 Patenting GPCRs and Other Proteins 3.8 The Four Horsemen of Patents: Patentable Subject Matter, Usefulness, Novelty, and Nonobviousness 3.8.1 Subject Matter: What Can Be Claimed? 3.8.2 Usefulness: Proving The Receptor ’s Function 3.8.2.1 Changes in the Utility Examination Guidelines 3.8.2.2 Meeting the New Utility Test: Characterizing Receptor Function 3.8.3 Novelty and Nonobviousness: Searching for Prior Art 3.8.3.1 Two More Horsemen: Adequate Written Descriptions and Enablement 3.9 Forging an IP-Savvy Business Model —Crafting IP-Savvy Operations 3.9.1 Managing the Tradeoffs 3.9.1.1 Tradeoff #1:Patenting Early vs. Patenting Strong 3.9.1.2 Tradeoff #2:Patent Strength vs. Patent Cost 3.9.1.3 Tradeoff #3:Litigation and licensing vs. the core business 3.9.2 Setting Up IP-Savvy Operations 3.10 When You Find Prior Art: Patenting a GPCR in the Face of Prior Discovery 3.10.1 Equivalent Inventions —The Impact of the Festo Case 3.11 Social Consequences and the Future of IP Law 4 Company Profiles 4.1 3-Dimensional Pharmaceuticals, Inc 4.1.1 Business Summary 4.1.2 Competitive Landscape 4.1.3 Product 4.1.3.1 ThermoFluor ® Screening Technology and HTS Enzymology 4.1.3.2 DirectedDiversity ® Combinatorial Chemistry Technology 4.1.4 Structure-Based Drug Design 4.1.5 Proteomica ™ GPCR Structural Genomics Database 4.1.6 Financials 4.2 7TM Pharma 4.2.1 Business Summary 4.2.2 Products 4.2.3 Financials/Investors 4.3 Aptus Genomics 4.3.1 Business Summary 4.3.2 Summary 4.3.3 Financials/Investors 4.4 Arena Pharmaceuticals 4.4.1 Business Summary 4.4.2 Product Pipeline. 4.4.2.1 Orphan Receptors 4.4.2.2 Known GPCRs 4.4.2.3 Other Receptor Families 4.4.3 Collaborations and Alliances 4.4.4 Competitive Analysis 4.4.5 Acquisition &Mergers 4.5 Atugen 4.5.1 Business Summary 4.5.2 Technologies 4.6 Aurora Biosciences, Inc 4.6.1 Business Summary 4.6.2 Products 4.6.2.1 Fluorescent Assay Technologies 4.6.2.2 Screening Platforms 4.6.3 Competitive Analysis 4.6.4 Collaborations/Customers (since December 2000) 4.7 Discovery Partners, Inc 4.7.1 Business Summary 4.7.2 Assay Development Services 4.7.3 Combinatorial Chemistry Instruments 4.7.4 Libraries 4.7.5 Chemistry Protocols 4.7.6 Drug Discovery Informatics 4.7.7 Financials 4.8 Euroscreen S.A. 4.8.1 Business Summary 4.8.2 Products 4.8.3 Competitive Landscape 4.8.4 Financials 4.8.5 Investors 4.8.6 Patents and Patent Applications 4.9 Exalpha BioPharmaceuticals, Inc. 4.9.1 Business Summary 4.9.2 Products 4.9.2.1 Theranostics 4.9.2.2 Theracept 4.10 LifeSpan Biosciences, Inc 4.10.1 Business Summary 4.10.2 Products 4.10.2.1 Drug Target Database 4.10.2.2 Target Validation Services and LifeSpan ’s Human Tissue Bank 4.10.2.3 Antibody Library 4.10.2.4 Pathology Services 4.10.3 Customers 4.10.4 Competitive Analysis 4.10.5 Financials 4.10.6 Investors 4.11 Molecular Devices, Inc 4.11.1 Business Summary 4.11.2 Drug Discovery Products 4.11.3 Life Sciences Research Products 4.11.4 Products 4.12 Norak Biosciences, Inc 4.12.1 Business Summary 4.12.2 Technology 4.12.3 Competitive Landscape 4.12.4 Financing/Investors 4.13 PerkinElmer, Inc 4.13.1 Business Summary 4.13.2 Products 4.13.2.1 AlphaScreen ™ and BRET2 ™® -Arrestin 4.13.2.2 Gene2Screen ™ 4.13.2.3 ReFocus ™ 4.14 Synaptic Pharmaceutical Corporation 4.14.1 Business Summary 4.14.2 Future Products Pipeline/Therapeutic Focus 4.14.2.1 Central Nervous System (CNS) Disorders 4.14.2.2 Metabolic Diseases 4.14.2.3 Urological Diseases 4.14.3 Competitive Analysis 4.14.4 Collaborations and Alliances