GPCRs at Discovery on Target 2026
- Dr. GPCR News
- Aug 26
- 4 min read
Join Dr. GPCR at Discovery on Target 2026 in Boston, where GPCR science runs right through the heart of modern drug hunting.
If you work in drug discovery or biotech, Boston in the fall is where the conversation happens. Discovery on Target returns September 28 to October 1, 2026, and this year GPCR science is woven into the broader Lead Generation Strategies program, sitting alongside covalent chemistry, DNA-encoded libraries, biophysics, and direct-to-biology.
For us, that is a feature, not a footnote. GPCRs do not live in isolation, and neither do the people working on them. Seeing GPCR programs share a room with the newest hit-finding and lead-generation approaches is exactly how the field moves forward.
Our founder, Yamina Berchiche, PhD, is honored to be chairing the Targeting GPCRs session on Wednesday, September 30. In the run-up to the meeting, she sat down with several of the scientists presenting and teaching this year to hear what they are bringing to Boston.
Speaker Spotlight
Ahead of the meeting, we sat down with four of the scientists presenting and teaching in the GPCR track this year. Here are our conversations.
Evan O'Brien, PhD, Johns Hopkins University
Dr. O'Brien runs a lab at Johns Hopkins that blends cryo-electron microscopy with protein dynamics to build something closer to a movie of GPCR allostery than a single snapshot. His talk digs into the molecular basis of partial agonism at the mu opioid receptor, using mitragynine pseudoindoxyl and a newly identified allosteric pocket to tune signaling like a rheostat.
In a result the field will enjoy, his team solved the same molecule bound in both the active and inactive states of the receptor, and the weak partial agonist still delivered meaningful pain relief in a mouse model. A great example of why what happens in the animal matters as much as what happens in the in vitro assay.
Hailong Zhang, PhD, Shanghai Yogar Therapeutics
Dr. Zhang is a structural biologist with more than two decades in small molecule research across oncology and metabolic disease.
At Discovery on Target he presents YJ-015, a G protein biased APJ agonist developed as an adjuvant to GLP-1 therapy. The idea is elegant: GLP-1 agonists drive rapid weight loss but can take muscle along with the fat, and YJ-015 is designed to preserve muscle while the weight comes off. It is a timely look at how receptor pharmacology can sharpen one of the most talked-about therapeutic areas in the field.
Kris Borzilleri, Pfizer
A familiar face from last year, Kris Borzilleri is a longtime discovery scientist at Pfizer who moved from soluble proteins into the membrane protein world, bringing a deep biophysics toolkit with her.
At Discovery on Target she is giving a talk on an NMR fragment screen against an orphan GPCR, describing how her team navigated hit follow-up to drive down compound potency.
She is also co-teaching a short course on biophysical methods for GPCRs, covering protein NMR, SPR, and whole-cell SPR microscopy. Catch her on both the podium and in the classroom.
Dr. Terry Kenakin, UNC and Head Instructor at Terry's Corner
Dr. Kenakin is teaching a brand-new full-day short course in Boston on Monday, September 28: "The End Game: From Lead Optimization to Drug Candidate Selection."
Six hours of instruction centered on the part of discovery where much of the attrition happens, once you actually have a compound in hand.
Expect deep, practical treatment of affinity and efficacy, allosteric protein function, early safety, ADME, kinetics, and real case studies of compounds that looked promising and failed in the clinic, with a clear eye on why.
As Dr. Kenakin puts it, the goal is to translate moving biological readouts into hard chemical terms that hold up and predict what a molecule will do in people.
Why Dr. GPCR Is in This Conversation
At Dr. GPCR, our mission is simple: connect the GPCR community, share knowledge, and accelerate innovation. Chairing the GPCR session at Discovery on Target is an extension of what we do every day, spotlighting strong science across academia and industry and bringing the people behind it together.
We are a nonprofit, and we have spent six years building a trusted, science-first space for this community. Stepping into the GPCR track at Discovery on Target is part of that work.
Inside the GPCR Track This Year
The GPCR content is concentrated on Wednesday, September 30, and it spans an unusually wide slice of the field:
Antifibrotic and anti-inflammatory targets, including GPR68
Biased ligand discovery and orphan receptors such as GPR75
Designer partial agonism at the mu opioid receptor
Small molecule approaches to obesity through GIPR
Muscle-sparing strategies for GLP-1-driven weight loss through APJ
Structural biology of the opioid receptors using single molecule FRET and cryo-EM
Fragment-based discovery for orphan GPCRs
Membrane mimetics and how the lipid environment shapes receptor behavior
There is also a morning roundtable on modern GPCR-targeted drug discovery, tackling which hit-finding strategies are actually delivering tractable GPCR leads, where AI and machine learning genuinely change the workflow, and which functional readouts teams trust enough to make go or no-go decisions.
Keep Learning with Terry's Corner
If you cannot get enough of Dr. Kenakin's teaching, Terry's Corner is our room where he breaks down receptor pharmacology, functional selectivity, and ligand bias in ways you can apply directly to your work. You can also sign up for the free weekly Kenakin brief delivered to your inbox at https://www.ecosystem.drgpcr.com/terry-corner#signuptc.
We have GPCR-focused courses coming this fall as well, so stay tuned.
Join Us in Boston
Discovery on Target, Boston, MA.
September 28 to October 1, 2026
Track: Lead Generation Strategies, with GPCR sessions on Wednesday, September 30
Use code GPCR26200 for $200 off the current registration rate as part of our collaboration with Discovery on Target.
Let's connect, let's debate, and let's keep moving GPCR drug discovery forward, together.
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