Insights That Move the GPCR Field Forward

Dear Dr. GPCR Community, If the past few years have been about finding our rhythm, this year has been about refining our systems — and stepping confidently into what’s next. When we started Dr. GPCR, it was with a simple goal: to connect people who shared a passion for GPCR science and discovery. What began as a small, volunteer-driven initiative has grown into a vibrant global network — thousands of scientists, founders, students, and partners who now learn, collaborate, a

The next edge in discovery isn’t louder exposure—it’s smarter engagement. This week’s Dr. Kenakin from Terry's Corner shows how to tame irreversible drugs so their kinetic power works for you, not against you. You’ll get a framework to predict duration, penetration, and PK/PD separation—so decisions move faster and risks surface earlier. Breakthroughs this week: nanomedicines targeting PAR2 for sustained analgesia; Emerging Voices in GPCR Biology;

Discover how Dr. Eric Trinquet, creator of HTRF and IP-One assays, turned failure into breakthrough tools for GPCR science. Learn why play, serendipity, and partnerships fuel innovation—and how this mindset can transform your research and biotech career.

Every drug you design will meet an enzyme before it meets its receptor. If you want your molecules to survive first contact with biology—and with the FDA—enzyme inhibition must be part of your core playbook. This week’s feature breaks down exactly how to think about inhibitors with rigor and speed, so you can make better decisions earlier in the pipeline. Breakthroughs this week: Potentiation of GPCR signaling by ATP and sugar monophosphates; Pharmacology 2025; Nxera Pharma

Before your GPCR ligand ever meets its receptor, it meets the enzymes that determine whether it survives long enough to act. Recognizing, predicting, and leveraging these interactions is the essence of enzyme inhibition pharmacology—the framework that connects molecular survival to clinical success.

If you want cleaner decisions, start with the system—then the ligand. This week’s lead feature unlocks a deceptively simple lever that separates signal from storytelling, moving programs forward with fewer surprises. That’s precisely what Terry’s Corner delivers: practical tools from Dr. Terry Kenakin to elevate your science and sharpe It’s a curated toolkit designed to help GPCR professionals move faster, with more confidence. Premium Members count on this every week—and t

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.

Choosing the right fluorescent tools is important for the success of drug discovery, just as much as choosing the right targets. One of the best tools to study therapeutic targets are fluorescent ligands, which are very useful in GPCR drug discovery, starting from hit and lead validation all the way to pre-clinical assays. Some of the advantages of using fluorescent ligands for this are

Boston, MA – September 2025 — Dr. GPCR, the global nonprofit platform dedicated to advancing GPCR science through education, community, and platform visibility, is proud to spotlight pHSense™, a new reagent family from Revvity, now featured across the Dr. GPCR Ecosystem.

Curve shifts can mislead, but statistics won’t. This week in Terry’s Corner: power analysis, t-tests, ANOVA, and F-tests to move from “I think” to “I know.” Plus, Ajay Yekkirala on AI-driven GPCR therapeutics and an invitation to Boston’s GPCR Happy Hour. Premium Members get full access to curated jobs, events, and must-read publications—your edge to stay ahead in fast-moving GPCR science.

This week's breakthroughs are crucial for staying ahead in the rapidly evolving landscape of GPCR research and drug discovery. Dr. Terry Kenakin's insights on target residence time can reshape how you evaluate and advance lead compounds, potentially saving your team from costly late-stage failures. That's exactly what Dr. GPCR delivers every week: practical tools and critical intelligence to elevate your science and sharpen your decisions.

Every September, Boston welcomes the global biotech and drug discovery community. Scientists, investors, and CRO professionals fly in from around the world, while Boston’s own vibrant life sciences hub shows up in full force. GPCR Happy Hour is where these two worlds meet. It’s not just networking. It’s where partnerships spark, ideas collide, and the GPCR community grows stronger — together.

GPCRs pose a critical challenge in drug discovery: a vast therapeutic potential with many targets yet to be explored.  35% of...

That’s why this week at Dr. GPCR, we’re focusing on the hidden risks that undermine progress and how the right frameworks can keep your pipeline moving forward.

In Terry Kenakin’s latest lecture from the Emerging Drug Hunter series, he invites you into a thought-provoking reevaluation of one of pharmacology’s most misleading concepts: the myth of high and low-affinity binding sites.

Is Your GPCR Program Slowing Down—Even With Good Data? You’re not alone. Most teams don’t stall because the science is weak. They stall...

Why I Started GPCR Consulting You've got great data. You've got brilliant scientists. But your GPCR program still isn't moving at the...

1.     Introduction 1.1 The Endocannabinoid System The Endocannabinoid System (ECS) is composed of the Cannabinoid Receptors 1 and 2...

Hello GPCR Minds,   This week, you'll learn all about Terry’s Pharmacology Corner, your new learning space focused on GPCR pharmacology. Whether you’re early in your career or pushing the edge of MoA design, weekly lesson help you apply key concepts like binding, signaling, and kinetics in practical, decision-shaping ways. The Corner comes will live monthly AMA sessions with Dr. Kenakin. Get curated content at your own pace.   Subscribe to The Kenakin Brief below to stay in t

Understanding receptor-ligand interaction is key in drug discovery and biomedical research. Radioligands have been used to study GPCRs...

Hello GPCR Trailblazers, This week, we’re spotlighting Celtarys Research, our newest partner, featured in a blog and podcast with CSO Dr. Maria Majellaro, highlighting their fluorescent ligand tools for live-cell GPCR assays.   After 40+ years and 250 publications, Dr. Terry Kenakin is launching a new learning space with video courses, AMAs, and practical insights . Get a sneak peek  and sign up for The Kenakin Brief—his free weekly newslette r.   On the industry side, Novo N

Celtarys Research Joins Dr. GPCR – Precision Tools for GPCR Assays Dr. GPCR and Celtarys Research have teamed up. This partnership aims to bring advanced chemical probe strategies to the forefront. The goal is to accelerate receptor-targeted discovery. They will showcase innovative conjugation methods. These methods will provide scientists with direct access to emerging tools and insights. Explore the partnership Multiplexing GPCR Discovery - Sakmar Lab’s Toolkit Goes Publi

1.       Introduction Dopamine receptors are G-protein-coupled receptors (GPCRs), which have 5 subtypes -D1-5. The dysfunction of these...

November 2022 "Neuropeptides produce robust effects on behavior across species, and recent research has benefited from advances in...