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GABAA (γ-aminobutyric acid, type A) receptors are targeted by numerous small-molecule drugs, many of which were discovered before their target was known. Using single particle cryo-electron microscopy (cryo-EM), the first structure of a GABAA receptor in a physiological conformation, reconstituted into a lipid bilayer, has been solved, as have five structures of the same receptor in complex with various drugs. These structures provide insights into the mechanisms of action of GABAA receptor-targeting molecules and could provide the basis for future structure-based drug discovery.