Mass spectrometry is one of the most widespread technologies in chemistry and has been increasingly used in biology with the rise of omics sciences. This book summarizes important mass spectrometry related methodological approaches and applications in the field of chemical biology. It provides an important compendium of theoretical and experimental techniques that can be applied to study a wide range of problems in biological systems and would therefore be of great interest to students and researchers in the fields of analytical chemistry, biochemistry and chemical biology.