Comprehensive Medicinal Chemistry, Fourth Edition provides a contemporary and forward-looking critical analysis and summary of recent developments, emerging trends, and recently identified new areas where medicinal chemistry is having an impact. The discipline of medicinal chemistry continues to evolve as it adapts to new opportunities and strives to solve new challenges. These include drug targeting, biomolecular therapeutics, development of chemical biology tools, data collection and analysis, in silico models as predictors for biological properties, identification and validation of new targets, approaches to quantify target engagement, new methods for synthesis of drug candidates such as green chemistry, development of novel scaffolds for drug discovery, and the role of regulatory agencies in drug discovery. A list of new areas covered includes: - newer assays, techniques, applications in medicinal chemistry - use of artificial intelligence and machine learning in drug discovery and development (prediction of drug efficacy, toxicity, and ADME properties, identification of new drug targets; design of novel drug candidates) - big data - chemical biology - degradation technologies - Precision medicine (targeted therapies; the use of biomarkers to guide drug development) Reviews the strategies, technologies, principles, and applications of modern medicinal chemistry Provides a global and current perspective of today's drug discovery process and discusses the major therapeutic classes and targets Provides a contemporary and forward-looking critical analysis and summary of cutting-edge technologies in drug discovery Chapters follow a consistent structure and feature elements such as key objective boxes, summaries, figures, methods, schemes, and tables