The 7‐chloro‐4‐(piperazin‐1‐yl)quinoline structure is an important scaffold in medicinal chemistry. It exhibited either alone or as hybrid with other active pharmacophores diverse pharmacological profiles such as: antimalarial, antiparasitic, anti‐HIV, antidiabetic, anticancer, sirtuin Inhibitors, dopamine‐3 ligands, acetylcholinesterase inhibitors, and serotonin antagonists. In the presented review, a comprehensive discussion of compounds having this structural core is surveyed and illustrated.