The Asinger multicomponent reaction is a versatile synthetic tool which gives access to multiple drug‐like scaffolds such as 3‐thiazolines. The diversity and easy access of its starting materials, its operational simplicity combined with mild conditions and relatively good yields, renders the Asinger reaction, today more than ever, a cornerstone not only in heterocyclic chemistry and modern synthesis but also in medicinal chemistry. In this review, we perform a thorough analysis of the scope and limitations on the different reaction variants with their starting materials, the three‐dimensional solid‐state conformations of the Asinger derivatives, and we underline and classify all the major post‐modifications that have been described. In addition, we report all the major applications in drug discovery projects. Titan of the toolkit: The Asinger multicomponent reaction can play an important role in drug design and discovery due to the diversity and complexity that offers. Here, we present the scope and limitations of the reaction, its orthogonal combination with classic or other MCRs and the applications in drug discovery. We believe that Asinger reaction will find its position in today's sustainable chemistry.