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 to
human physiology
and highly
druggable targets
*Nature Reviews Drug Discovery, Volume 214, June 2025, 458-479
Strong relevance across multiple therapeutic areas
Axxam delivers integrated GPCR discovery solutions.
Translating complex GPCR biology into actionable drug discovery insights.
~80
Human GPCR targets, several assays already available for clients
~400
odorant receptors + TAS1R (sweet/umami) + TAS2R (bitter)
HTS- and compound testing-ready assays for:
- Agonists
- Antagonists
- PAMs
- AMP (Gs/Gi) — HTRF, GloSensor, CNG
- Ca²⁺ (Gq) — GCaMP, dye-based assays, IP1-HTRF
- β-arrestin — NanoBiT, PathHunter®
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.
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..
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
PAM
characterization
Kd determination
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.
