2-Aminopyridine is a simple, low molecular weight and perfectly functionalised moiety known for the synthesis of diverse biological molecules. Many pharmaceutical companies across the globe aim to synthesise low-molecular weight molecules for use as pharmacophores against various biological targets. 2-Aminopyridine can serve as a perfect locomotive in the synthesis and pulling of such molecules towards respective pharmacological goals. The major advantage of this moiety is its simple design, which can be used to produce single products with minimum side reactions. Moreover, the exact weight of synthesised compounds is low, which enables facile identification of toxicity-causing metabolites in drug discovery programmes. This manuscript is a quick review of such pharmacophores derived from 2-aminopyridine.