Author: Peter Norman, MBA, PhD
Executive Summary
Chapter 1
INTRODUCTION
1.1. Overview
1.2. Declining Innovation
1.3. Difficult Targets
Chapter 2
CHEMICAL CONSIDERATIONS
2.1. Introduction
2.2. The Impact of HTSChemical Libraries
The Rule of 5 (Lipinski)
Molecular Obesity
2.3. Chemical SpaceDrug Space
2.4. FragmentsFragments as Leads
What Are Suitable Fragments?
Rule of 3
Ligand Efficiency and Lipophilic Ligand Efficiency
2.5. Fragment LibrariesCharacteristics
Size
Chapter 3
SCREENING APPROACHES
3.1. Introduction
3.2. In Silico Methods
3.3. Surface Plasmon Resonance Methods
3.4. NMR ScreeningSolution Phase
Solid Phase
3.5. X-Ray Methods
3.6. Mass Spectral Methods
3.7. Isothermal Calorimetry
3.8. Capillary Electrophoresis
3.9. Microfluidic Assays
3.10. Other Approaches
3.11. Bioassays
3.12. Overview
Chapter 4
CASE HISTORIES
4.1. Introduction
4.2. Abbott's Bcl Inhibitors
4.3. Astex' Kinase Inhibitors
4.4. Heptares' Adenosine A2a Antagonists
4.5. Vernalis' Hsp90 Inhibitors
4.6. Vemurafenib
4.7. Conclusions
Chapter 5
SPECIALIST COMPANIES
5.1. Introduction
5.2. Alveus Pharmaceuticals
5.3. Astex Pharmaceuticals
5.4. Beactica
5.5. BioFocus
5.6. BioLeap
5.7. CRELUX
5.8. Crown Biosciences
5.9. Emerald BioStructures
5.10. Evotec
5.11. Graffinity
5.12. Heptares
5.13. Iota Pharmaceuticals
5.14. Kinetic Discovery
5.15. NovAliX
5.16. Nuevolution
5.17. Polyphor
5.18. Proteros Fragments
5.19. Pyxis Discovery
5.20. Selcia
5.21. Silicos
5.22. Sprint Bioscience
5.23. Structure Based Design
5.24. Sygnature Discovery
5.25. Vernalis
5.26. Viva Biotech
5.27. Zenobia Therapeutics
5.28. ZoBio
Chapter 6
OUTLOOK
6.1. Introduction
6.2. New Methods
6.3. Corporate InterestMajor Companies
Other Companies
6.4. Development Compounds
6.5. Conclusion
Chapter 7
RESULTS FROM INSIGHT PHARMA REPORTS' FRAGMENT-BASED SCREENING SURVEY
7.1. Survey Description
7.2. Survey Analysis
7.3. Survey Results
References
Glossary
Company Index