Insights That Move the GPCR Field Forward

Discovery on Target returns to Boston September 28 to October 1, 2026, with GPCR science woven through the Lead Generation Strategies program. Ahead of the meeting, we spoke with four scientists presenting and teaching this year, from partial agonism to obesity targets to fragment screening against orphan receptors.

We tend to call a GPCR antibody “validated,” as if the question were settled. The GeneTex team makes the case for a humbler word, characterized, and for handing the hardest reagents in receptor biology back to the researchers who use them.

On April 29, GPCR scientists filled Pressed Cafe in Boston for the first Dr. GPCR Happy Hour of 2026. No slides, no panels, just the conversations that usually happen in hallways or never at all. Here is what the night looked like, and why it is exactly why this community exists.

Drug discovery is built on a seductive simplification: identify the malfunctioning receptor, design a compound that engages it, and restore function. But many diseases don't cooperate with that assumption. Alzheimer's, metabolic disease, psychiatric pharmacology — each carries evidence of multi-receptor architecture. Multi-target GPCR pharmacology is not a workaround. In certain disease architectures, it is the pharmacologically correct approach.

GPCR biologic drugs stabilize receptor active states through distributed contact networks small molecules have trouble reproducing. The affinity-trap account, treated as a model rather than a verdict, explains a recurring difficulty at family B GPCR programs.

GPCRs are one of the most important families of therapeutic targets in the pharmaceutical industry. They are involved in several pathologies, ranging from neurological, oncological, degenerative, metabolic, immunological… around a third of the drugs in clinical use are GPCR ligands

Binding affinity appears straightforward: add ligand, measure signal, fit a curve. Yet discovery teams routinely lose time and misallocate resources because the underlying biology behaves nothing like the idealized systems we learned in textbooks. GPCRs couple, decouple, isomerize, deplete tracers, and shift apparent affinity depending on stoichiometry and time. The result is a recurring pattern across programs—clean data that is not actually telling the truth. Orthosteric bi

When David Hodson’s lab teamed up with chemist Johannes Broichhagen aka JB (then a young researcher newly arrived during a home DIY moment), the goal was bold and elegant: Create a photo-switchable ligand to remotely control GPCR signaling with light. This was the moment when photopharmacology felt like the future. The literature was buzzing. Labs were competing. The idea was simple — turn signaling on or off with a flash of light.

When you walk into a typical academic lab, the boundaries are obvious: this PI’s corner, that group’s benches, their grants, their silos. But in Melbourne, a quiet experiment challenged that model — and it worked.

The first time Michelle ran a cyclic AMP assay, she did it with a single-channel pipette, trays of melting ice, and the kind of focus that only comes from knowing one mistake could waste weeks of work.

Michelle hadn’t mapped out a scientific empire. She was a student expecting tedium, not inspiration. Yet that summer research placement cracked open a new reality: the thrill of asking questions no one else could answer.

This week’s insights give you a strategic edge across the pipeline—from drug design that accounts for physiological counterforces, to simplifying internalization detection without microscopy, to boosting HTRF assay sensitivity using fluorescent ligands. It’s a curated toolkit designed to help GPCR professionals move faster, with more confidence. Premium Members count on this every week—and this is your preview.

Ajay Yekkirala’s journey from rejected med student to GPCR biotech founder shows how failure, mentorship, and curiosity can drive real innovation in drug discovery.

This week's Terry's Corner with Dr. Terry Kenakin delivers a game-changing framework for teams grappling with the gap between in vitro potency and in vivo performance.

Dr. Alex Serafini turned chronic pain into a research mission. Discover how personal experience shaped his work on GPCRs, RGS proteins, and new pain models.

October 2022 "Type 2 bradykinin receptor (B2R) is an essential G protein-coupled receptor (GPCR) that regulates the cardiovascular system...

September 2022 "G protein‐coupled receptors (GPCRs) are valuable therapeutic targets for many diseases. A central question of GPCR drug...