GPCR activation was historically viewed as a simple transition from one inactive to one active state. In reality, during activation, GPCRs progress through multiple conformational intermediates, which are rate-limiting and pharmacologically decisive.
Rational drug design, therefore, requires more than knowledge of endpoint function or endpoint structure. It requires linking ligand chemotype to all individual conformational intermediates that determine receptor activation.
Conformational Sequencing (ConfoSeq) is the first high-throughput platform to resolve structure-activity relationships across discrete receptor activation intermediates. By making those hidden states experimentally accessible at scale, ConfoSeq achieves drug discovery’s longest-sought ambition: the deterministic design of pharmacology.

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Illum Biotech

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