Engineering GPCR medicines, state by state

Illum Biotech is building a new generation of GPCR medicines using Conformational Sequencing, our proprietary drug-discovery platform.

ConfoSeq™ reveals how the molecular structure of ligands controls each step of receptor activation. We use these mechanistic design rules to discover differentiated medicines with precisely defined efficacy, signalling bias and selectivity through a proprietary pipeline and selected biopharma partnerships.

From empirical screening to designed pharmacology

GPCR drug discovery still relies largely on endpoint assays that compress receptor activation into a single downstream readout. These assays show the final response, but conceal the intermediate receptor states that produced it and the chemical features that control them. This hidden biology makes efficacy, signalling bias and subtype selectivity difficult to engineer rationally. Illum makes these pharmacologically decisive states measurable and actionable.

Conformational Sequencing

ConfoSeq™ is a state-resolved GPCR drug-discovery platform that operates at the plasma membranes of living cells.

ConfoSeq™ lies at the intersection of structure-based drug discovery and structure-activity relationships. It quantifies dose-response relationships for individual receptor conformations and links ligand molecular structure to each step of the receptor activation pathway. The resulting state-resolved structure-activity relationships reveal design rules that conventional functional assays and static structures cannot provide. ConfoSeq™ transforms receptor activation from an aggregated endpoint into a molecular design space.

ConfoSeq™ has been scaled for industrial drug discovery and validated across Class A and Class B GPCRs in collaboration with leading pharmaceutical companies.

A proprietary data advantage

Each ConfoSeq™ program produces mechanistically labelled data linking molecular structure, receptor conformation and functional response in the appropriate cell type.

As this dataset grows across chemical series and GPCR families, it creates a foundation for increasingly predictive models of efficacy, signalling bias and selectivity, and a compounding advantage for future discovery programs.

Mission

Engineer new GPCR drugs with superior therapeutic profiles. Create valuable drug assets through selected partnerships with biotechnology and pharmaceutical companies and a proprietary pipeline.