DREADDs: novel tools for drug discovery and development

•DREADD is the acronym for Designer Receptors Exclusively Activated by Designer Drugs.•Available DREADDs are activated by the inert ligand clozapine-N-oxide.•DREADDs allow for exquisite fine-tuning of signaling pathways.•DREADDs are novel and useful tools in the discovery and development of drugs targeting GPCRs.

Since the invention of the first designer receptors exclusively activated by designer drugs (DREADDs), these engineered G protein-coupled receptors (GPCRs) have been widely applied in investigations of biological processes and behaviors. DREADD technology has emerged as a powerful tool with great potential for drug discovery and development. DREADDs can facilitate the identification of druggable targets and enable researchers to explore the activities of novel drugs against both known and orphan GPCRs. Here, we discuss how DREADDs can be used as novel tools for drug discovery and development.