Deterministic design of GPCR pharmacology

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, each of which can be rate-limiting and pharmacologically decisive.

Rational drug design, therefore, requires more than knowledge of endpoint function or endpoint structure. It requires linking 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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  • Our mission is to turn the pharmacology of GPCR drugs from an empirical outcome into a design variable, helping pharmaceutical companies accelerate drug discovery across therapeutic areas.

  • GPCR activation is a sequence of intermediate conformational steps. Conventional signalling assays collapse that sequence into a single downstream output. As a result, the structure-activity relationships that govern efficacy, signalling bias, and subtype selectivity remain largely hidden. This is the central reason that GPCR pharmacology remains difficult to design rationally.

  • ConfoSeq is a high-throughput assay that quantifies dose-response relationships for individual receptor conformations in the plasma membrane of living cells. It reveals state-resolved structure-activity relationships across the activation pathway and turns hidden intermediates into decision-ready pharmacology.

    This is not an incremental improvement to a downstream assay. It is a new measurement layer for GPCR drug discovery.

  • ConfoSeq Profiling
    State-resolved pharmacology for compound libraries, reference ligands, and chemical series. Designed for hit triage, lead ranking, comparative profiling, and early assessment of efficacy, bias, and selectivity.

    ConfoSeq Rapid Rational Design and Optimisation
    A DMTA-aligned collaboration model for teams that want to engineer pharmacology, not simply describe it. Use ConfoSeq to co-design libraries, rescue overlooked chemistry, and optimise efficacy, pathway bias, receptor subtype selectivity, and context selectivity.

  • Partners receive more than assay data. They receive conformation-resolved dose-response maps, state-resolved SAR, mechanistic interpretation of compound behaviour, and clear decision packages for subsequent chemistry cycles.