We offer a broad perspective of this rapidly-expanding interdisciplinary field, ranging from seminal classical experiments to state-of-the-art tools to perturb and probe living systems. With each lecture topic dedicated to discussing one recent publication in the field, the course exposes students to real-world scientific literature and data evaluation. Through these case examples, the course emphasizes the need for careful design and responsible execution of chemical-biology experiments, including ways to avoid pitfalls. Wherever applicable, benefits and limitations of modern chemical-biology methods are addressed and contrasted against classical genetic and biochemical/cell biological techniques.