GPCR Drug Discovery at Discovery on Target: Why This Track Is About More Than Receptors

Join Dr. GPCR and global experts at the GPCR Drug Discovery session during Discovery on Target 2025—where groundbreaking collaborations begin.

GPCR Drug Discovery at Discovery on Target 2025 — The Track You Can’t Miss

If you work in drug discovery or biotech, this is your moment.

Mark your calendar, it's happening September 22-25, 2025.

From obesity and diabetes to cancer, fibrosis, and CNS disorders — GPCRs are at the heart of the world’s most pressing therapeutic challenges. And at this year’s Discovery on Target meeting in Boston, the GPCR Drug Discovery track will deliver breakthroughs, bold ideas, and the strategies shaping the next wave of medicines.

I’m honored to be chairing a session in this track — with none other than Terry Kenakin on the speaker lineup.

🌐 Why Dr. GPCR Is in This Conversation

At Dr. GPCR, our mission is simple: connect the GPCR community, share knowledge, and accelerate innovation. At Yamina's Corner,I work closely with organizations to help them navigate receptor pharmacology, identify opportunities, and move their programs forward effectively.

Over the years, we’ve built a global network of researchers, biotech leaders, and pharma innovators who believe that GPCR science is one of the most powerful tools we have to address urgent health challenges.

Chairing this session isn’t just another speaking engagement — it’s an extension of what we do every day:

• Spotlight innovation across academia and industry.

• Foster collaboration through our platform and events.

• Push the boundaries of receptor pharmacology and its real-world applications.

When we step into the GPCR track at Discovery on Target, we’re not just participating. We’re helping shape the conversation.

🚀 Why GPCRs Are Still the Hottest Target Class in Drug Discovery

GPCRs regulate countless physiological processes, making them a goldmine for therapeutic breakthroughs. They’re already behind blockbuster drugs:

• GLP-1 receptor agonists – reshaping obesity & type 2 diabetes care.

• CCR5 antagonists – fighting HIV and certain cancers.

• Dopamine D2 receptor modulators – transforming treatment for Parkinson’s & schizophrenia.

• PAR1 antagonists – protecting cardiovascular health.

But the real excitement is in what’s next:

• Biased signaling for selective therapeutic effects.

• Allosteric modulation for unprecedented precision.

• Structure-based design powered by cryo-EM and AI.

🔬 Inside the GPCR Track Agenda

Expect deep dives into:

• CXCR4 in oncology and immune regulation.

• GIPR/GLP-1R co-agonists in metabolic diseases.

• Serotonin & dopamine receptor modulation for neuropsychiatric disorders.

• Orphan GPCRs with untapped therapeutic potential.

These sessions bridge structural biology, computational modeling, and clinical translation — with tangible takeaways for programs from discovery through late-stage development.

🌟 Speaker Spotlight

In the run-up to the conference, our founder Yamina Berchiche is speaking with some of the brilliant minds presenting in the GPCR track.

Here’s who we've talked to so far:

🎥 Interview with Dr. Aaron McGrath from Takeda (Coming Soon)

🎥 Interview with Kris Borzilleri & Alison Heick Varghese from Pfizer (Coming soon)

We'll continue to update this section as new videos are released — so check back before the meeting for fresh insights and behind-the-scenes perspectives from our speakers.

🗝️ Highlight: Terry Kenakin at Discovery on Target

Terry Kenakin’s work on functional selectivity has transformed GPCR drug discovery, showing how to bias receptor signaling toward beneficial outcomes and away from side effects.

Hearing Terry speak is more than an academic experience — it’s like being handed a new set of tools to rethink your drug design strategy. Having him in the session I’m chairing is not just an honor — it’s a highlight of the year.

 

📚 Terry’s Corner — The Only On-Demand Pharmacology Hub with Dr. Kenakin Himself

If you’re part of the Dr. GPCR community, you already know about Terry’s Corner — our exclusive, on-demand pharmacology series where Terry Kenakin breaks down receptor pharmacology, functional selectivity, and ligand bias in a way you can apply directly to your work.

It’s the only resource of its kind — part masterclass, part fireside chat — available anytime to our members. For those who can’t get enough of Terry’s insights at Discovery on Target, Terry’s Corner keeps the learning going long after the conference ends.

💡 Why This Matters — Even If You’re Not a GPCR Scientist

GPCR pathways intersect with oncology, CNS, metabolic, cardiovascular, immunology, and fibrosis research. Whether you’re in early discovery or clinical development, the strategies here could open doors in your own therapeutic area.

🧭 Join Us in Boston

🗓 Discovery on Target — Boston, MA

📅 September 23-25, 2025

🎯 Track: GPCR Drug Discovery

Let’s connect. Let’s debate. Let’s move GPCR drug discovery forward — together.

🚨 Mark your calendar for the GPCR Happy Hour

Join us at GPCR Happy Hour, where scientists, biotech leaders, CRO professionals, and investors from around the globe meet Boston’s vibrant life sciences hub.

✨ Spark collaborations.

✨ Strengthen the GPCR community.

✨ Be part of Dr. GPCR’s nonprofit mission to connect and empower the global GPCR ecosystem.

📅 September 24, 2025

📍 Pressed Café, Huntington Ave, Boston

⏰ 6–8 PM EST

⚠️ Space is limited — Secure your spot now