Includes bibliographical references and index.

1. Natural products as a discovery resource -- Chemical diversity and genetic equity: synthetic and naturally derived compounds -- Microcollection of plants for biochemical profiling -- Enzymes and microbes as a source of chemical diversity -- The marine environment as a discovery resource -- 2. Compound sourcing: chemically generated screening libraries -- Rapidly expanding molecular diversity: libraries from libraries -- Synthesis of encoded small molecule combinatorial libraries via ECLiPS -- Parallel organic synthesis using Parke-Davis' Diversomer method -- Rapid discovery and optimization of biologically active small molecules using automated synthesis methods -- CMT: a solution phase combinatorial chemistry approach: synthesis and yield prediction of phenazines -- Design of a diverse screening library -- Automating combinatorial chemistry: challenges and pitfalls -- Combi-chem high throughput screening for leads optimization -- 3. Assay technologies and detection methods -- Bioassay design and implementation -- Scintillation proximity assays -- FlashPlate technology -- Assays for small molecule agonists and antagonists of the neurotrophin receptors -- A homogeneous, time-resolved fluorescence method for drug discovery -- Time-resolved fluorometry: advantages and potentials -- Adaptation of time-resolved fluorescence to homogeneous screening formats -- Fluorescence polarization -- Reporter gene assay applications -- Development of a gene expression-based screen using quantitative polymerase chain reaction -- High-performance microphysiometry in drug discovery -- Bio-analytical applications of BIAcore, an optical biosensor -- 4. Automation and robotics -- Management and service issues of a centralized robotic HTS core -- Flexible use of people and machines -- Bar-code technology and a centralized database: key components in a radioligand binding program -- Factors for the successful integration of assays, equipment, robotics, and software -- Accelerating the discovery process with automation and robotics: a sure bet or a risky venture? -- Perspectives on scheduling -- 5. Data retrieval, handling and integration -- Database systems -- Systems integration -- Data management and tracking for natural product programs. -- 6. Laboratory design and management -- Planning and implementing an HTS program -- Establishing an HTS program in a start-up biotechnology company.