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Science Spyglass Why do GPCRs continue to dominate drug discovery? A central drug discovery target class. GPCRs sit at the centre of human physiology and remain among the most druggable proteins we have. 516 approved drugs target GPCRs — about 36% of all medicines 121 distinct GPCR targets already addressed by approved drugs 151 GPCR targets currently in clinical trials Central tohuman physiologyand highlydruggable targets *Nature Reviews Drug Discovery, Volume 214, June 2025, 458-479 Strong relevance across multiple therapeutic areas Neurology Immunology Oncology Cardiovascular Respiratory Metabolic Axxam capabilities. Axxam delivers integrated GPCR discovery solutions. Translating complex GPCR biology into actionable drug discovery insights. Receptor expertise ~80 Human GPCR targets, several assays already available for clients ~400 odorant receptors + TAS1R (sweet/umami) + TAS2R (bitter) Functional assays HTS- and compound testing-ready assays for: Agonists Antagonists PAMs Functional readouts AMP (Gs/Gi) — HTRF, GloSensor, CNG Ca²⁺ (Gq) — GCaMP, dye-based assays, IP1-HTRF β-arrestin — NanoBiT, PathHunter® Translating complex GPCR biology into actionable drug discovery insights. Webinar The Critical Importance of GPCR Functional Assays in Drug Discovery Projects Explore how GPCR functional assays and in vitro pharmacology can help characterize drug candidates beyond potency, predict their activity across biological systems, and identify potential safety and ADME limitations early in drug discovery. Designing the right assays to identify GPCR hits. Every GPCR routes its signal through one or more of three main functional pathways. Reading the right one is what turns a screen into usable pharmacology. cAMP Ca²⁺ β-arrestin 1. Confirm biological activity Is the activity real? A functional readout separates genuine target engagement from assay noise. 2. Identify the signaling pathway Which pathway is being activated? Matching the assay to the receptor’s native coupling matters. 3. Prioritize the best candidate Which hit should move forward? Functional data ranks candidates on more than potency alone.. Beyond the hit. Finding GPCR hits isn’t the hardest part. Understanding them is. A confirmed hit still leaves open how it behaves at the receptor. These five characterizations fill in that picture. Schild analysis Biased signaling Residence time PAMcharacterization Kd determination Actionable pharmacology data for better candidate selection Putting it together. From complex GPCR biology to confident drug discovery decisions Functional assay development Pharmacological characterization Hit-to-lead support End-to-end expertise to de-risk and accelerate GPCR programs Let’s discuss your GPCR discovery project Bring us your target, your hits, or your toughest GPCR question.We’ll help you build the assay strategy to investigate it. From assay development to compound characterization: Develop robust functional assays Screen agonists, antagonists and PAMs Characterize compounds beyond potency Generate data for confident decisions Have a GPCR challenge in mind? Tell us about your target, compounds or assay needs. Discuss your GPCR project Back