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GPCR Drug Discovery Summit 2026: What to Expect in Boston — and How to Register

Dr. GPCR × GPCRs-Targeted Drug Discovery Summit text, with logos, set on white background. Event in Boston, April 28–30.


Dr. GPCR is proud to partner with the 5th Annual GPCRs-Targeted Drug Discovery Summit. This post is your one-stop hub — agenda highlights, who's attending, our exclusive discount code, and speaker interviews as they go live.



Why the GPCR Drug Discovery Field Is Converging in Boston


The GPCR field is in a genuinely exciting moment. Not hype — momentum. The human genome encodes ~800 GPCRs, yet only around 15% are currently targeted by approved drugs — leaving an enormous and largely untapped therapeutic opportunity.


New structural tools, AI-driven design pipelines, and a growing number of programs moving into the clinic are redefining what's possible across modalities and indications. Pharma interest is high, as reflected in major deals across the space.


The 5th Annual GPCRs-Targeted Drug Discovery Summit is the industry-led meeting dedicated entirely to GPCR drug discovery — across small molecules, peptides, and antibodies, and across indications. This year's program reflects where science is actually heading.


Dr. GPCR founder Dr. Yamina Berchiche will be there — if you're attending, reach out to connect.



Who's at the GPCR-Targeted Drug Discovery Summit 2026


The meeting brings together 80+ senior leaders from biotech and pharma to advance GPCR programmes from discovery through translation — experts in GPCR biology, structural biology, computational design, pharmacology, and translational strategy.


Companies already confirmed to attend include:


Abalone Bio  ·  AbbVie  ·  Biagon  ·  Biolexis Therapeutics  ·  Confo Therapeutics  ·  Eli Lilly  ·  GSK  ·  Nabla Bio  ·  Northeastern University  ·  Nxera Pharma  ·  OMass Therapeutics  ·  Superluminal Medicines  ·  Tectonic Therapeutics  ·  and many more.



GPCR Drug Discovery Agenda Highlights: What's New in 2026


This year's summit runs across three days — an AI & ML Focus Day on April 28, followed by two conference days — and the program spans the full breadth of the field.



Biased Signaling, Endosomal Pathways & GPCR Signaling Complexity


How do we disentangle intrinsic, system, and kinetic bias in a way that actually predicts clinical outcomes? Sessions from InterAx Biotech, Northeastern University, and Function Therapeutics dig into this — moving beyond static potency and efficacy to mechanistic signatures that guide drug design. A panel discussion will tackle best practices for measuring GPCR signaling bias in vitro and what that means for in vivo and clinical translation.


AI & ML in GPCR Drug Discovery


A dedicated focus day brings together teams from Nabla Bio, Abalone Bio, Biagon, Iambic Therapeutics, Lembas, and Eli Lilly. These aren't primers on AI — they're teams presenting real workflows and real data, covering generative antibody design, dynamic conformational modeling, federated computing platforms, and predictive simulations that shorten discovery timelines.


Antibodies, Cyclic Peptides & Allosteric Modulators


Nine or more presentations on non-small molecule approaches — including agonistic antibodies, GPCR-directed ADCs, orally available cyclic peptides, and allosteric probes for Class B GPCRs. Companies presenting include Skymab Biotherapeutics, Confo Therapeutics, GSK, Metaphore Biotechnologies, and Abilita Therapeutics.


Translational Stories & Clinical Data


OMass Therapeutics on long-residence MC2R antagonists. Tectonic Therapeutics on engineering a long-acting relaxin for pulmonary hypertension. Kainova Therapeutics presenting Phase 1 outcomes for their EP4 receptor antagonist in solid tumors. Alphamol on Phase 1 results from an orphan GPCR program pursued against industry skepticism.



🎥 Speaker Spotlight: GPCR Drug Discovery Experts to Watch (coming soon)


In the run-up to the summit, we're speaking with some of the researchers presenting at the meeting. We'll be adding interviews here as they go live — check back for updates.



Register for the GPCR Drug Discovery Summit — Exclusive DrGPCR Discount


Use the exclusive DrGPCR discount code DRGPCR10 at checkout for 10% off registration. Early bird pricing also runs through March 6, saving up to $600 off the door price — so don't wait.


  🔗  Register here


The 5th Annual GPCRs-Targeted Drug Discovery Summit takes place April 28–30, 2026 at The Colonnade, 120 Huntington Avenue, Boston, MA.

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