Asymmetric organocatalysis became one of the principal methods for the catalytic synthesis of chiral compounds. This thematic issue in the Beilstein Journal of Organic Chemistry aims to highlight new developments across all subdisciplines of enantioselective organocatalysis. This timely collection of articles deals with methodological advances in both covalent (enamine, iminium, phosphine, carbene, etc.) and noncovalent organocatalytic activations, which are often connected to developments of new catalysts. Important mechanistic and computational studies deepen our understanding of this topic and the underlying processes. The gradual maturation of this field is demonstrated by applications of its methodologies to target molecules synthesis, such as natural products or compounds of medicinal interest.