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Designing covalent allosteric modulators brings brand new opportunities to the world of medicine breakthrough towards G-protein-coupled receptors (GPCRs). Focusing on an allosteric binding pocket can allow a modulator to have protein subtype selectivity and low drug weight. Using covalent warheads further makes it possible for the modulator to raise the binding potency and increase the timeframe of action. This review begins with GPCR allosteric modulation to talk about the architec