Description |
1 online resource (314 pages) |
Series |
RSC Drug Discovery |
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RSC drug discovery series.
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Contents |
880-01 Cover ; Fragment-Based Drug Discovery; Foreword ; Preface ; Contents; Personal Essay: Fragments in the Blogosphere; 1 Introduction; 2 A Living Review; 3 Warning Signs and Guideposts; 4 A Mirror for the Community; 5 Beyond Practical Fragments: Fragments in the Broader Social Media; Acknowledgements; References; Personal Essay: Adventures and Experiences in Fragment-Based Drug Discovery; 1 In the Beginning; 2 We are all Brought up to be Fragment Practitioners; 3 Setting up Fragment Screening at RiboTargets/Vernalis; 3.1 Targeting Hsp90 |
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880-01/(S 4 The Future of Fragment-Based Methods -- The Future is Now4.1 Challenging Targets; 4.1.1 β-Site Amyloid Precursor Protein Cleaving Enzyme 1; 4.1.2 G Protein-Coupled Receptors; 4.1.3 Protein-Protein Interactions; 4.1.4 Allosteric Site Inhibitors; 4.2 Progress in the Absence of Crystal Structures; 4.3 New, Novel Different Fragments; 5 Fragment Discovery Outside Industry; 6 Summary; References; Chapter 1 -- Different Flavours of Fragments; 1.1 Fragment-Based Drug Discovery; 1.2 Different Types of Fragments; 1.3 How We Identify Fragments; 1.4 Selectivity; 1.5 Applications of Fragment-Based Methods |
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1.5.1 Assigning Function1.5.2 Assessing Ligandability; 1.5.3 Speeding Up Chemical Validation; 1.6 Targeting Protein-Protein Interactions and Beyond; 1.7 Targeting Oligonucleotides; 1.8 Concluding Remarks; References; Chapter 2 -- Getting the Most Value from Your Screens: Advances in Hardware, Software, and Methodologies to Enhance Surface Plasmon Resonance Based Fragment Screening and Hit-to-Lead Support; 2.1 Introduction; 2.2 SPR Technology as Applied to FBS; 2.3 The Basic Screening Cascade; 2.4 Advances in Data Reduction and Active Selection in Primary Screening |
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2.4.1 Robust Drift Correction by Local Estimation2.4.2 Method #1 for Hit Detection: Box Plots; 2.4.3 Method #2 for Hit Detection: Normal-Exponential Convolution Model; 2.4.4 Implementation and Automation in R; 2.5 High-Throughput Competition Experiments for Binding Site and MOA Studies; 2.5.1 Configuring SPR-Competition Assays; 2.5.2 A Quantitative Specificity Metric for Selecting Competitive Compounds; 2.6 Hardware Improvements; 2.6.1 SensiQ Pioneer Hardware and Novel Types of Injections; 2.6.2 Screening by Gradient Injections: Hardware and Software Integration; 2.7 Conclusions; References |
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Chapter 3 -- Applications of NMR in Fragment-Based Drug Design3.1 Introduction; 3.2 Ligand-Observed Experiments; 3.2.1 STD Experiments; 3.2.1.1 Principle and Experimental Conditions; 3.2.1.2 Recent Pulse Sequence Development; 3.2.1.3 STD as a Tool for Fragment Screening and Fragment Ranking; 3.2.1.4 STD as a Tool for Binding-Mode Assessment; 3.2.2 WaterLOGSY Experiments; 3.2.2.1 Principle and Experimental Conditions; 3.2.2.2 Recent Pulse Sequence Development; 3.2.2.3 WaterLOGSY as a Tool For Fragment Screening and Fragment Ranking; 3.2.2.4 WaterLOGSY as a Tool for Binding-Mode Assessment |
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3.2.3 Other Applications of STD and WaterLOGSY Experiments |
Summary |
This book will prove to be an invaluable resource for medicinal chemists working in academia and industry, as well as anyone interested in drug discovery techniques |
Notes |
English |
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Print version record |
Subject |
Drug development.
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Ligands (Biochemistry)
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Ligands.
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Pharmaceutical chemistry.
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Chemistry.
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Pharmacology.
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Life sciences.
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Physical sciences.
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Drug Discovery
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Ligands
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Chemistry, Pharmaceutical
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Laboratory Chemicals
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Investigative Techniques
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Specialty Uses of Chemicals
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Analytical, Diagnostic and Therapeutic Techniques and Equipment
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Chemistry
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Pharmacology
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Biological Science Disciplines
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Natural Science Disciplines
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Chemical Actions and Uses
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Chemicals and Drugs
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Disciplines and Occupations
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chemistry.
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pharmacology.
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biological sciences.
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physical sciences.
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Physical sciences
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Pharmacology
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Pharmaceutical chemistry
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Ligands
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Life sciences
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Chemistry
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Drug development
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Ligands (Biochemistry)
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Form |
Electronic book
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Author |
Drysdale, Martin
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Erlanson, Daniel A
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Giannetti, Tony
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Krimm, Isabelle
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Hann, Michael
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Kutchukian, Peter
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Hughes, Terry
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Spry, Christina
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De Esch, Iwan
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ISBN |
1849739080 |
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9781849739085 |
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9781782620938 |
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1782620931 |
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