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;

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

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

Each edition highlights the decisions that move GPCR projects forward—from pharmacology essentials to ligand binding site strategies, bench-ready tools, and industry momentum shaping GPCR pipelines. Read fast, apply faster, and stay ahead in GPCR drug discovery with evidence-based insights—no hype, just strategies you can use.

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.

Early signals can mislead. This week’s Dr. GPCR Weekly shows how to call Mechanism of Action with model-first rigor—distinguishing orthosteric vs. allosteric, designing assays that reveal mechanism, and unlocking SAR. Plus: Novo’s \$550M obesity/diabetes push, Rhythm’s sNDA, key events, and confocal imaging that respects function. Upgrade to Premium for the full digest.

Early signals can mislead. This week’s Dr. GPCR Weekly shows how to call Mechanism of Action with model-first rigor—distinguishing orthosteric vs. allosteric, designing assays that reveal mechanism, and unlocking SAR. Plus: Novo’s \$550M obesity/diabetes push, Rhythm’s sNDA, key events, and confocal imaging that respects function. Upgrade to Premium for the full digest.

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 Dr. GPCR Weekly News delivers urgent insights every GPCR scientist and drug discovery leader needs. From Terry’s Corner on the hidden traps of allosteric binding, to Yamina’s Corner on the hidden costs of fragmented systems, and a preview of Discovery on Target 2025, this edition highlights the frameworks shaping the next decade of therapies. Plus: industry breakthroughs on metabolic GPCRs, key September events, curated career opportunities, and must-read publicat

Join us at the Discovery on Target meeting in Boston for the GPCR Drug Discovery track! I’m honored to chair a session featuring Terry Kenakin, a leader in functional selectivity. We’ll explore GPCR targets like GLP-1R, CXCR4, and dopamine receptors across oncology, metabolic, CNS, and immunology. As Dr. GPCR, we connect scientists and accelerate innovation — see you in Boston!

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.

In pharmacology, the wrong interpretation of antagonist behavior can derail your conclusions, your experiments, and even your program’s credibility. That’s why mastering competitive vs non-competitive antagonism isn’t optional — it’s essential for accurate, defensible science. This week’s Terry’s Corner takes you beyond curve shapes into the kinetic and mechanistic realities that separate surface-level analysis from true expertise.

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.

Allostery isn’t just an advanced concept—it’s essential to understanding efficacy, ligand bias, and receptor behavior in real-world systems.

Welcome GPCR Fans,   Every discovery-phase decision you make shapes your entire pipeline trajectory—and understanding when equilibrium...

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.

The latest Terry’s Corner unlocks clinical forecasting tools few scientists truly master.

Welcome Back, Discovery Drivers   Terry’s Corner is live, on-demand pharmacology built for drug discovery. Yamina’s Corner opens for strategic consulting, and our partner Celtarys unveils a robust TR-FRET assay for CBRs. Plus: must-read chemokine and PTH1R papers, and new momentum across biotech—from Superluminal to Neurocrine to novel GLP-1 contenders. Dr.GPCR Updates Terry’s Corner is Live - Pharmacology at your fingertips Terry’s Corner is now open! Explore 10 on-demand l

Terry’s Corner — a new platform where GPCR scientists can sharpen their thinking, expand their toolkit, and learn directly from Dr. Terry Kenakin. Ten on-demand courses are live now, built to challenge assumptions and bring clarity to the complex, evolving world of GPCR pharmacology.

Hello GPCR Innovators ,   We’re preparing to launch Terry’s Corner, a new knowledge hub shaped by Dr. Terry Kenakin’s decades of GPCR insight. It will bridge foundational receptor theory with today’s most pressing pharmacological questions, from biased signaling to allosteric design.   Meanwhile, incretin and amylin-based therapies are reshaping the obesity drug landscape. Novo Nordisk’s amycretin showed up to 24% weight loss, CagriSema delivered 22.7% in Phase 3, and semaglu

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

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

Dr. GPCR, the global knowledge hub for G protein-coupled receptor (GPCR) research and education, is proud to welcome Celtarys Research to its partner ecosystem. This collaboration aims to amplify the visibility and adoption of Celtarys’ cutting-edge fluorescent ligand technology and accelerate the development of GPCR-targeted therapeutics.