Library Synthesis and Quality Control -- Using a Noncovalent Protection Strategy to Enhance Solid-Phase Synthesis -- Quality Control of Solid-Phase Synthesis by Mass Spectrometry -- Preparation of Encoded Combinatorial Libraries for Drug Discovery -- Simple Tools for Manual Parallel Solid Phase Synthesis -- Cleavage of Compounds from Solid Phase by Gaseous Reagents -- Synthesis of DNA-Binding Polyamides -- The Preparation of Phenyl-stilbene Derivatives Using the Safety Catch Linker -- Host-Guest Chemistry -- Automated Structure Verification of Small Molecules Libraries Using 1D and 2D NMR Techniques -- Rapid Liquid-Phase Combinatorial Synthesis of Heterocyclic Libraries -- Soluble Polymer-Supported Methods for Combinatorial and Organic Synthesis -- Analytical Methods for Optimization and Quality Control of Combinatorial Synthesis -- Library Purification and Screening -- Resolving Racemic Mixtures Using Parallel Combinatorial Libraries -- Ligand Libraries for the Extraction of Metal Ions -- Automated Liquid-Liquid Extraction and Ion-Exchange Solid-Phase Extraction for Initial Purification -- On-Bead and Solution Screening Approaches for Genomically Derived Targets -- Computational Library Design -- Design of Virtual Combinatorial Libraries -- Approaches to Library Design for Combinatorial Chemistry -- Reagent-Based and Product-Based Computational Strategies in Library Design -- Designing Combinatorial Libraries for Efficient Screening -- Application of Neural Networks to Large Dataset QSAR, Virtual Screening, and Library Design.

By significantly increasing the number of targets available for drug discovery, the Human Genome and Proteome projects have made the use of combinatorial libraries essential to developing and optimizing drug candidate molecules more rapidly. Lisa English and a panel of expert researchers have collected in Combinatorial Library Methods and Protocols a novel series of computational and laboratory methods for the design, synthesis, quality control, screening, and purification of combinatorial libraries. Here the reader will find cutting-edge techniques for the preparation of encoded combinatorial libraries, for the synthesis of DNA-binding polyamides, and for combinatorial receptors. There are also state-of-the-art methods for computational library design, quality control by mass spectrometry, and structure verification using 1D and 2D NMR. A variety of well-known computational approaches are provided to meet the information management challenge of multiple biological assays. Each readily reproducible technique includes detailed step-by-step instructions and helpful notes on troubleshooting and avoiding pitfalls. Timely and highly practical, Combinatorial Library Methods and Protocols makes available for all drug discovery researchers all the powerful combinatorial chemistry tools that are increasing the number of candidate compounds and speeding the process of drug discovery and development today.