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Hi GPCR Fanatics,   This week’s insights will help you avoid wasted time, poor forecasts, and stalled programs. Let’s get you moving with confidence. 🔍 Quick Wins This Week 🔹 Tell us what matters → News Survey Your 1-minute feedback shapes what we spotlight next week. Help us help you. 🔹 Elevate your strategy → Building clarity in GPCR drug discovery Even the strongest GPCR programs stall—not from bad data, but from buried decisions; Yamina's Corner helps teams cut through the noise and build clarity that drives action. 🔹 Innovate faster → Celtarys’s newest GPCR tools Explore new screening tools purpose-built for speed and signal specificity. 🔹 Spot the opportunity → Why Catalio is betting big when others pull back Amid biotech slowdowns, Catalio’s contrarian investments offer insight into what’s next. Terry's Corner - New Course on Pharmacologic Models The latest Terry’s Corner unlocks clinical forecasting tools few scientists truly master.   ✅ Avoid costly errors:  Master vital models to confidently forecast outcomes, before it’s too late. ✅ Future-proof your career: Conquer complex laws and understand where receptor theory is going next. ✅ Premium Members:  Access your exclusive discount in the full newsletter   Secure Your Access Now ➤ 🗣️ “Thank you for bringing this (Principles of Pharmacology I) course with Dr. Kenakin. I wish Dr. GPCR the best for the sake of promoting more educational opportunities that are sorely needed in the field” — Dr. GPCR University Learner Dr. GPCR Podcast - Surviving Discovery’s Gauntlet Dr. Sokhom Pin delivers brutally honest insights.   Break stagnation:  Apply lessons from BMS, Novartis, Cerevel & more. Find your edge:  Dodge the traps that derail real drug discovery careers.   Listen Now – Real Lessons from a GPCR Expert ➤ The future of GPCR isn’t waiting. Get ahead, stay relevant, and lead—starting today.   The Dr. GPCR Team Read Full Edition ➤

Welcome GPCR Fans,   In GPCR-targeted drug discovery, precision isn’t optional—it’s a requirement. But precision isn’t just about clean data; it’s about interpreting what that data means. Subtle misinterpretation can quietly derail projects, slow timelines, and waste scarce resources. 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. This is a preview of what Premium Members access every week: industry insights, event updates, jobs, and classified publications—curated for scientists who need fast, actionable intelligence. 🔍 This Week in Premium: Sneak Peek Dr. GPCR Premium Members this week gain curated, early access to: Industry insights : GPCRs and mRNA in drug discovery; new strategies for inflammatory disease treatment; growth strategies from Tectonic Therapeutics Upcoming events : Lab-in-the-Loop AI-powered hit discovery (July 29); 5th Transatlantic GPCR Symposium (Sept 3–4); neuroGPCR Symposium (Sept 17) Career opportunities : Lead/Senior Researcher at St. Jude; Postdoctoral Fellow at University of Copenhagen; PhD in proteomics and GPCR signaling in cancer at CRCM Must-read publications : AlphaFold3 benchmarking for GPCRs; new structural insights into peptide ligand activation All curated for speed, relevance, and immediate application—only for Premium Members. Terry’s Corner: Rethinking Affinity, A Critical Edge for Drug Hunters One of the most persistent misconceptions in pharmacology workflows? The interpretation of high and low affinity binding sites on GPCRs. At first glance, when a ligand binds at two different affinities in the same system, it seems logical to assume two distinct sites. But Terry Kenakin’s new Emerging Drug Hunter lecture reveals why this assumption can mislead even experienced teams . What’s Really Going On? Under certain experimental conditions, what appears to be a second high-affinity site may simply reflect kinetic factors—such as ligand-receptor-G protein complex formation—creating the illusion of multiple sites that aren’t physiologically relevant. This misunderstanding leads to: Inefficient structure-activity relationship (SAR) cycles Wasted optimization efforts Focus on leads that fail later in development In this exclusive session, Kenakin gives you the frameworks needed to interpret data correctly, eliminate wasted effort, and accelerate confident decisions. 🔒 Available only in Terry’s Corner - Premium Members get an exclusive discount Secure Your Access To Terry's Corner ➤ Why the Myth of Multiple Affinity Sites Slows You Down Traditional models that shaped affinity analysis were designed for simpler systems. If you’re not accounting for their limitations today, your team risks costly misinterpretations that delay optimization cycles and waste resources. Kenakin shows exactly how to separate what matters from what misleads—practical, real-world expertise designed to help teams move faster, smarter, and with greater confidence. Every day spent misunderstanding apparent affinity differences delays key milestones. 🗣️ “Thank you for bringing this (Principles of Pharmacology I) course with Dr. Kenakin. I wish Dr. GPCR the best for the sake of promoting more educational opportunities that are sorely needed in the field” — Dr. GPCR University Learner Celtarys Research Recap: Medicinal Chemistry Highlights You May Have Missed The pace of innovation in medicinal chemistry is accelerating—and if you missed this year’s ACSMEDI-EFMC Medicinal Chemistry Frontiers 2025 , you’re already behind. At this international meeting, leaders shared next-gen strategies shaping modern drug discovery: Prof. Ingo Hartung : State-of-the-art design of small molecule drugs, including PROTACs Dr. Wendy Young : Career insights and lessons from a leader in drug development and a champion for women in science Dr. Katerina Leftheris : New technologies overcoming peptide limitations with insights from both pharma and startup environments Read Maria Majellaro's Full Recap ➤ Lab Leadership Without Ego: A Model for R&D Success Scientific rigor doesn’t thrive in cultures defined by micromanagement or burnout. At Alkermes, Sokhom Pin built an in vitro pharmacology group from scratch—not just a lab, but a culture that encouraged curiosity, empowered people, and supported balance while delivering results. His leadership principles: Hire for attitude and team fit—not just credentials Design workflows that enable curiosity-driven research Support work-life balance without compromising scientific excellence His approach didn’t just create a productive lab—it accelerated outcomes and laid the cultural foundation for the next generation of biotech innovation. Get The Full Story ➤ Why Dr. GPCR Premium Membership Gives You an Edge Dr. GPCR Premium is designed for scientists who need the right intelligence, fast—without noise, distractions, or delays. Every week, members get: A full edition of GPCR Weekly News : jobs, events, papers, industry updates Exclusive discounts on Terry’s Corner  digital pharmacology courses Priority access to insights from major conferences, emerging research, and expert commentary Whether you’re a pharmacologist, biotech scientist, or team leader, Dr. GPCR Premium gives you an edge in a fast-moving field. FAQ: What’s Included, Who It’s For, Why Now What’s included? The complete Weekly News digest, jobs, upcoming events, classified industry intelligence, Courses, & Conference Presentations. Who is it for? Scientists, drug discovery teams, and pharmacologists who need curated, career-relevant updates. Why now? The field is evolving rapidly. Those acting on the right insights now will define the next wave of discovery. Don’t Fall Behind—Access the Edge You Need 👉 Access all the news and upcoming events ➤ Already a Premium Member? Access this week’s full Premium Edition here ➤ Hashtags: #GPCR #DrGPCR #BindingAffinity #Pharmacology #DrugDiscovery #LeadOptimization #TerryKenakin #EmergingDrugHunter #EfficientDiscovery #PipelineAcceleration

Masterclass on GPCR Allostery: Unveiling Techniques to Decode Drug Behavior – July 31st, 2025. Welcome back GPCR fans, If your drug discovery strategy still relies on static GPCR models, you’re already behind. Allostery isn’t just an advanced concept—it’s essential to understanding efficacy, ligand bias, and receptor behavior in real-world systems. That’s exactly what Terry’s Corner delivers this week: high-impact insight into GPCR allostery, crafted for pharmacologists and biotech scientists who need to translate mechanistic nuance into better decision-making. 🔍 This Week in Premium: Sneak Peek Industry insights:  Strategic biotech alliances (Chemspace/Enamine, Superluminal Medicines), Novartis financial leadership shakeup, and next-gen GPCR targeting platforms reshaping immunotherapy pipelines. Upcoming events:  GPCR-UK Network Meeting, neuroGPCR symposium, and Transatlantic ECI GPCR event—where discovery and collaboration intersect. Career opportunities:  Exclusive pharma and academic listings you won’t find on job boards—curated for translational scientists and GPCR specialists. Must-read publications:  CXCL12 dimer impact on AML migration, mechanosensitive behavior in GPCRs, and in vivo APLNR biosensor imaging. Terry's Corner : Stop Chasing Affinity and Start Reading the System In this week’s cornerstone Terry’s Corner lecture, Dr. Terry Kenakin reframes GPCRs as dynamic, allosteric sensors—far from static binding sites. This is the lens that lets scientists anticipate drug effects, decode kinetic behavior, and optimize probe-dependent signaling. What you’ll learn: Reveal cryptic binding sites and time-dependent interactions.  Some drugs take hours to reach equilibrium—not because of poor design, but because the system is fluid. Learn how to decode that fluidity. Exploit probe dependence to shape precision pharmacology.  Want to avoid off-target effects? Understand how GPCRs react differently depending on the probe. Map dynamic receptor behavior to real-time decision-making.  Allostery is not passive—it’s predictive. Leverage this model to stay ahead of therapeutic complexity. To stay in the know on upcoming courses and AMA session, get the complementary Kenakin Brief , the weekly newsletter delivered directly to your inbox. Sharpen your discovery decisions ➤ GPCR Signal Transduction Call for Papers: Define What Comes Next Volume I was just the beginning with over 28K reads. As the GPCR field surges forward—from ligand bias to signaling diversity—the guest editors Dr. Lauren Slosky, Stuart Maudsley and Yamina Berchiche invite your insights for Volume II. This is a chance to shape the next scientific consensus on how GPCRs work, signal, and fail. Why this matters: Secure your voice in the next chapter of GPCR science.  Your work belongs in the core conversation—not buried in supplementary files. Position your research for maximum visibility.  This is where funders, peers, and biotech scouts are watching. Contribute to an evolving field still rich with firsts.  Volume II isn’t about repetition—it’s about redefining signal transduction. 📝 Manuscript summary deadline: 23 Sept 2025 📄 Submission deadline: 11 Jan 2026 Submit to Volume II ➤ Discovery On Target: Where the Next Decade of GPCR Drugs Begins If you’re not attending the GPCR-focused sessions at Discovery On Target 2025, you’re missing where the field is headed. It’s the 20th anniversary—and the spotlight is squarely on kinetic modeling, allosteric frameworks, and targeting the “undruggable.” 🔥 Featured:  Dr. Terry Kenakin on “The Kinetics of Allostery: The Added Benefits of Allosteric Function.” Why you need to be there: Learn how kinetic nuance shapes ligand design.  Don’t just measure residence—understand it. Access peer insights on allosteric modulators and biased ligands. Join the conversation on computational targeting and next-gen selectivity. Register for Discovery On Target ➤ What our community is saying “I enjoy the breadth of questioning that goes beyond just the science, and reveals a bit about the scientists as individuals/mentors/people.” — Dr. GPCR Podcast Listener Why Dr. GPCR Premium Membership Gives You an Edge Premium delivers curated, noise-free intelligence every week: deep-dive expert lectures, classified industry news, priority event alerts, job opportunities, and insider commentary—designed to help you move faster, smarter. If you work on GPCRs across translational pharmacology, drug development, or molecular pharmacology, this is your decision advantage. Our Premium Members don’t have to chase signals—they act on them. FAQ: What You Get with Dr. GPCR Premium 🔹 What’s included? The complete Weekly News digest, curated jobs, upcoming events, classified GPCR publications, exclusive on-demand expert frameworks, and member-only discounts. 🔹 Who is it for? GPCR scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who need fast, curated, career-relevant intelligence to stay ahead. 🔹 Why now? The pace of GPCR innovation is accelerating. Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won’t see coming. 👉 Access all the news and upcoming events ➤ 👉 Already a Premium Member?  Read the Full Edition here ➤

Exploring Intracellular Targets: Bridging the Gap Between In Vitro and In Vivo GPCR Research - August 7th, 2025. Welcome back GPCR fans, The pace of GPCR innovation is accelerating at a rate that can be difficult to keep up with. For drug discovery teams and scientists, staying ahead requires more than just reading papers—it demands access to the right frameworks and expert insights that separate the noise from the signal. That’s exactly what Terry’s Corner delivers every week: practical tools from Dr. Terry Kenakin to elevate your science and sharpen your decisions. Breakthroughs this week: Glucagon-like Peptide-1 Receptor (GLP-1R) Signaling; Proximity-Dependent Proteomics; Multicolored sequential resonance energy transfer. 🔍 This Week in Premium: Sneak Peek Don't miss the key insights and opportunities that are shaping the future of GPCR research and drug discovery right now. This week's Premium content offers a curated look at what's moving the industry and scientific community forward. Industry insights:  Crinetics' Palsonify gains momentum in acromegaly, a key indicator for pipeline expansion; Septerna's chart signals upward expansion; and a look at how chronic diseases are driving growth in the global GPCR targeting market. Upcoming events:  Get details on the "neuroGPCR" symposium focusing on receptor signaling and a platform for unlocking "undruggable" targets with AI-powered hit discovery. Career opportunities:  New openings for a postdoctoral research position in GPCR biochemistry and biophysics and a research associate/scientist in in vitro pharmacology. Must-read publications:  A deep dive into proximity-dependent proteomics of adenylyl cyclase isoforms, a case for functionally Gs protein-selective GPCRs, and new methods for detecting simultaneous ligand binding. Terry's Corner : Unlock the Power of Intracellular GPCR Drugs For years, GPCR drug discovery has focused on targets at the cell surface. But what if the most significant opportunities lie just inside the cell membrane? This week Dr. Terry Kenakin delivers a game-changing framework for teams grappling with the gap between in vitro potency and in vivo performance. His latest lecture is a guide to understanding why intracellular drug access changes everything—from target residence time and rebinding kinetics to the discovery of previously untargetable sites. Solve the in vitro/in vivo disconnect:  Understand why traditional potency measurements often fail to predict clinical success and learn how intracellular kinetics can provide the missing link. Gain a competitive edge:  Learn to leverage restricted diffusion and rebinding to create drugs with longer therapeutic coverage, even with shorter systemic exposure. Avoid missed opportunities:  Discover how to identify and target cryptic intracellular allosteric sites, opening up new avenues for "failed" or under-studied GPCRs. To stay in the know on upcoming courses and AMA session, get the complementary Kenakin Brief , the weekly newsletter delivered directly to your inbox. Sharpen your discovery decisions ➤ Dr. GPCR Podcast : The Future of GPCR Drug Discovery with Molecular Modeling The field of GPCR research is being transformed by the accessibility of computational tools. In this week's Dr. GPCR Podcast, we sit down with Alessandro Nicoli, from the Technical University of Munich, to discuss his work on olfactory receptors. He shares his journey into computational chemistry and offers a compelling look at how tools like AlphaFold are providing new starting points for drug discovery. Learn how his research aims to develop models that can distinguish between active and inactive ligands, paving the way for computational ligand discovery even where experimental data is scarce. Harness the power of AI:  Discover how breakthroughs like AlphaFold are making previously "undruggable" targets, like olfactory receptors, accessible for computational analysis. Bridge the gap between disciplines:  Get practical advice from a computational expert on how wet-lab scientists can integrate computational tools like Python and Talktorials into their work. Learn from a pioneer:  Hear how mentorship and team science are fueling innovation in the field and providing a path for the next generation of GPCR scientists. Expand your computational toolkit ➤ Call for Papers: GPCRs: Signal Transduction, Volume II Building on the success of its first volume, the research topic "GPCRs: Signal Transduction: Volume II" is now open for submissions. This is a critical opportunity for the scientific community to come together and share new findings on how GPCRs regulate bodily functions, health, and disease. This research topic is designed to stimulate discussion and fuel the scientific direction of future GPCR research within the field of Cellular Biochemistry. Amplify your research:  Contribute to a high-impact collection of work that will shape the future of GPCR signaling studies. Connect with experts:  Join a community of like-minded field-experts dedicated to improving our collective understanding of GPCRs in human health. Stay ahead of the curve:  Showcase your latest findings on the essential role GPCRs play in disease and their function as important drug targets. Discover the research topic ➤ Why Dr. GPCR Premium Membership Gives You an Edge Staying at the forefront of GPCR science is not just a goal—it’s a necessity. The right information at the right time can mean the difference between a breakthrough and a dead end. Dr. GPCR Premium Membership delivers curated, noise-free intelligence every week: deep-dive expert lectures, classified industry news, priority event alerts, job opportunities, and insider commentary—designed to help you move faster, smarter, and with greater confidence. This isn’t just a newsletter; it's a strategic tool for your career and your science. “The best pharmacology teacher (Dr. Kenakin) teaming up with the best GPCR community platform to help train and inspire the next generation of scientists. Also super-valuable for those of us learning how to teach pharmacology” — Dr. GPCR Course Attendee FAQ: What You Get with Dr. GPCR Premium What’s included?  The complete Weekly News digest, curated jobs, upcoming events, classified GPCR publications, exclusive on-demand expert-led courses, and member-only discounts. Who is it for?  GPCR scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who need fast, curated, career-relevant intelligence to stay ahead. Why now?  The pace of GPCR innovation is accelerating. Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won’t see coming. Don’t Fall Behind—Access the Edge You Need 👉 Access all the news and upcoming events ➤ 👉 Already a Premium Member?  Read the Full Edition here ➤ The field of GPCRs is dynamic and competitive. To succeed, you need to move beyond standard approaches and adopt the frameworks that are driving real innovation. Dr. GPCR Premium Membership gives you direct access to the experts and insights that can redefine your work. Don’t wait for others to lead—become a Premium Member today and access the intelligence that will power your next breakthrough.

Watch Episode 171 Some careers are planned. Alessandro Nicoli’s wasn’t. Born near Venice and trained as a pharmaceutical chemist, Alessandro never imagined himself working at the cutting edge of computational GPCR research. But one academic spark—and the right mentor—changed his trajectory forever. In this blog post, we dive into his story of scientific curiosity, chance opportunities, and the unlikely road that led him to the Technical University of Munich. The Early Days: Molecules and Mentors Alessandro began his academic life studying pharmaceutical chemistry at the University of Padua. While fascinated by organic chemistry and the idea of “building molecules,” he didn’t see the big picture—until he encountered Prof. Moro , a medicinal chemist who introduced him to the interplay between molecular structure and biological function. “It was not just a molecule—it was a partner interacting with a protein or DNA… that opened a new world.” —Alessandro Nicoli This perspective changed everything. Suddenly, chemistry wasn’t just synthetic—it was strategic. He began exploring how small modifications could radically alter biological outcomes, an insight that later fueled his move toward computational research. Falling for Computational Chemistry Alessandro’s master’s thesis brought him face to face with his “second academic love”: computational chemistry . Studying cancer-related proteins (BCL2 family), he combined NMR and molecular docking to explore drug candidates. The realization that he could ask—and answer—complex biological questions with a computer sealed the deal. “Doing every day the results, I was getting in love with the topic and decided—yeah, I want to do this in my life.” —Alessandro Nicoli After graduation, a serendipitous email from Prof. Moro led him to an opportunity in Prof. Antonella Di Pizio’s lab  in Munich. Within weeks, he moved to Germany and became her first PhD student—helping build a lab from the ground up. From Empty Lab to GPCR Discovery Starting in an empty lab with just a shared desk, Alessandro and Antonella began their mission: to computationally study olfactory GPCRs , a massively under-characterized group of receptors. With hundreds of subtypes and limited ligand data, olfactory GPCRs represent a high-risk, high-reward challenge —perfect for a PhD built on curiosity and courage. “Choosing one specific receptor is difficult… they’re unique because they can bind many different molecules. Let’s embrace the challenge to study all of them.”  —Alessandro Nicoli Want to explore computational GPCR science yourself? Explore the   GPCR University  or enroll in Terry's Corner for GPCR Courses led by Dr. Terry Kenakin. ________ Keyword Cloud: #GPCRresearch #DrugDiscovery #ComputationalChemistry #MolecularModeling #MolecularDynamics #AlphaFold #StructuralBiology #InSilicoBiology

Watch Episode 170 Thinking Differently Pain research has long followed a familiar route: from molecule, to cell, to animal, to human. But as Dr. Alex Serafini  explains, this conventional bottom-up approach often fails to deliver therapies that truly help patients, especially in the pain field. In his work, Serafini emphasizes a phenotype-driven, patient-relevant perspective , where animal models closely mirror human experience before mechanistic reductionism begins. This approach reflects his focus on developing models that behave  like patients before molecular exploration takes over. "I'm particularly interested in model development... seeing if we can bring preclinical models much closer to the actual human experience than what we're using now." Learning from COVID-19 One striking example came from his COVID-19 work during his PhD. Rather than starting with a molecular hypothesis, Serafini’s team noticed that hamsters infected with SARS-CoV-2 exhibited persistent pain-like behaviors . This observation triggered deep RNA-seq profiling and new hypotheses. This patient-centric and behavior-first approach uncovered robust gene expression signatures  linked to pain, without being constrained by pre-existing assumptions about which molecular players to interrogate. Why This Approach Matters In pain research, bottom-up approaches often fail to translate. Drugs that look great in vitro fall apart in humans. By starting with phenotype-first studies , Serafini’s approach offers a translational lens more tightly aligned with clinical realities. He also integrates concepts like sex differences , epigenetic inheritance , and neuroimmune crosstalk  — factors often absent in reductionist models. This allows him to see how inflammation, cognition, and pain circuits overlap , and how GPCRs might serve as more responsive therapeutic nodes. A Call for Patient-First Science Serafini’s strategy isn’t just about method — it’s about mindset. It asks researchers to consider the entire ecosystem: from patient to molecule , not just the other way around. And it challenges the GPCR community to use its tools not just to explain, but to intervene. Takeaway We don’t need better in vitro data — we need better models of reality. Dr. Alex Serafini makes the case for building pain research from the clinic down, not the bench up. ________ Keyword Cloud: GPCR podcast , pain modeling , GPCR online course , translational research , neuroimmune signaling .

Imagine testing a molecule, seeing no response, and shelving it. But what if your system just wasn't sensitive enough  to see what it was really doing? In this eye-opening module, Terry Kenakin explores a concept that could change how you interpret pharmacological data: the interplay between intrinsic efficacy and system sensitivity. It’s not just about what your molecule does —it’s also about how capable your system is at showing it. Through powerful analogies (think batteries and balance scales), Terry reveals why different tissues—and even different assays—can paint totally different pictures of the same  compound. The result? Misinterpreted potency. Missed opportunities. And potential drug candidates left behind. From oxymetazoline to oxotremorine, discover how drugs can show up as full agonists in one system and antagonists  in another. If you're an emerging drug hunter, this lesson is your bridge from data confusion to predictive clarity. 👉 Dive into Terry’s Vault and see agonism like never before Unlock "Agonism & Sensitivity" now

Imagine running a calcium assay and discovering your compound shows only weak activity. What if that result wasn’t telling you the whole story? In this foundational lesson, Terry Kenakin dives deep into a widely used, often misunderstood tool in early drug discovery: the calcium assay. Revered for its convenience, the FLIPR assay provides rapid insights into receptor activity. But its speed comes with a cost. You’ll learn why calcium signals are inherently transient—giving rise to a “hemi-equilibrium” window that can significantly distort your understanding of drug potency. Through real-world examples (like 5-HT2A and CCR5 agonists), Terry shows how slow-onset agonists can be drastically underestimated—potentially leading promising leads to be dismissed too early. Why does this matter? Because when true pharmacological profiling is essential—like detecting partial or inverse agonism—calcium assays just don’t deliver. If you're starting out in pharmacology, this lesson gives you the interpretive tools to ask smarter questions, avoid missteps, and use calcium assays with strategic clarity. 📍 Foundational Level | Calcium Assays 📚 Part of Terry Kenakin’s Pharmacology Vault 👉 Curious what else you've been missing? Unlock "Calcium Assays" now

Imagine you're navigating a vast terrain—not on foot, but through the shape-shifting world of GPCRs. What if the static models we've relied on for decades have been hiding the truth? In this exclusive Expert Drug Hunter lesson, Terry Kenakin dismantles 100 years of receptor theory and introduces you to a dynamic new framework: Molecular Dynamics. Discover how receptors actually behave, how ligands uniquely sculpt their function, and how cryptic allosteric sites are quietly reshaping the frontier of drug discovery. This isn’t just theory, it’s a practical revolution. With the right lens, you’ll see why efficacy is more than signal strength: it's a fingerprint of conformational selection. 📍 Ready to think beyond the textbook? Step into Terry’s Vault and explore “Molecular Dynamics”—where expert drug hunters forge the future. 🔓 Access the Vault. Understand the Movement. Unlock “Molecular Dynamics” Now

Are you ready to truly understand how pharmacologists predict whole-body drug response from a single experiment?   Terry Kenakin’s newest foundational lesson in Terry's Corner  cuts straight to it:   Why models are vital for translating lab data into clinical forecasts The 4 types of pharmacologic models (and when to use each) The truth about linear models: useful or misleading? How the Mass Action Law underpins nearly every model Future of Receptor Theory: Linkage vs. Probability Models   This is practical drug development expertise from Terry’s 40+ years of experience.   Beyond the lessons, Terry's Corner  is your exclusive gateway. Ecosystem Premium Members: Look for significant savings on this and other resources in your weekly Dr. GPCR News.   Elevate your pharmacology expertise. Unlock "Pharmacologic Models" now

Watch Episode 170 What We’re Missing in Pain Research In GPCR drug discovery, receptors typically steal the spotlight. But as Dr. Alex Serafini  pointed out in his interview, Regulators of G protein Signaling (RGS proteins)  might hold some of the most untapped therapeutic opportunities, particularly in pain neuroscience. Serafini described his connection to GPCRs as tangential but inevitable: "I feel like I never was particularly explicitly interested in GPCR signaling... but the thing about GPCRs... is you always kind of end up landing at a GPCR as a major target." His work in the lab of Dr. Venetia Zachariou  introduced him to the power of RGS proteins — particularly RGS4  — in modulating pain circuits in ways that traditional targets fail to capture. RGS4 and the Unexpected Recovery Phenomenon One of the most compelling findings in Serafini’s experience was the spontaneous recovery observed in RGS4 knockout mice . “There was this very interesting phenotype the lab found where, as a mouse was starting to enter what we consider the chronic pain range, the mice that were constitutively RGS4 knocked out started recovering spontaneously. And this is a recovery that is very rare to see at the preclinical level. " Such recovery is rare in preclinical pain models and hints that RGS proteins could modulate pain chronification itself . These findings suggest a path forward that isn’t about blocking a single receptor but about rewiring the entire system upstream of pain perception. Serafini noted that RGS4 was especially intriguing because it was expressed robustly both in the peripheral nervous system and in central circuits like the prefrontal cortex and thalamus  — areas deeply involved in both pain perception and affective comorbidities. GPCRs in the Background, But Always Present Even though his primary focus wasn’t GPCRs themselves, Serafini repeatedly encountered them as unavoidable players in pain-related pathways. Whether working on opioid withdrawal, addiction vulnerability, or chronic pain, GPCR-related signaling repeatedly emerged as the core mediator  — demonstrating the reach of these signaling pathways beyond classical receptor pharmacology. This realization isn’t isolated. Serafini highlighted that in modern pain drug development, the field has remained too focused on ion channels like NAV1.8 , despite these targets falling short clinically: “The downstream cascade is probably a little bit weaker than if you were hitting a GPCR... and honestly, like with the trials, they were not really that sufficiently better than opioids, right? And in itself, that's kind of a suggestion.” Takeaway Forget what you think you know about GPCR drug targets. The real power may lie in how they’re regulated. Dr. Serafini’s work on RGS proteins suggests a quieter, but no less powerful, frontier in the fight against chronic pain. ___________ Keyword Cloud: RGS4 , GPCR data platform , GPCR training program , pain research , opioid signaling .

Welcome GPCR Fans,   Every discovery-phase decision you make shapes your entire pipeline trajectory—and understanding when equilibrium affinity falls short is no longer optional. That’s exactly what Terry’s Corner  delivers this week: real-world kinetic frameworks to help you move faster and make smarter choices. Breakthroughs this week: Structure-based discovery of positive allosteric modulators of the A1 adenosine receptor; GPR171 is necessary for normal physiological functions and mood-related behaviors in males, but not females; Discovery on Target GPCR Drug Discovery. 🔍 This Week in Premium: Sneak Peek A curated preview of this week’s Premium classified content — designed to keep you ahead without noise or delays: Industry insights:  Structure-Based Drug Design Summit; AI-Powered GPCR Research; Lab-in-the-Loop Hit Discovery advances. Upcoming events:  5th MMCS New Trends in Drug Discovery; GPCR-UK Network Meeting; neuroGPCR Symposium. Career opportunities:  Principal Scientist - In Vitro Pharmacology; Senior Scientist, Molecular Pharmacology; PhD position in proteomics and GPCR signaling. Must-read publications:  GPCRchimeraDB: Database of engineered GPCR designs. All curated for speed, relevance, and immediate application—only for Premium Members. Terry’s Corner: Why Binding Kinetics Matter More Than Affinity In drug discovery today, time wasted is opportunity lost. Yet too many programs rely solely on affinity metrics—Kd—as proxies for in vivo behavior, missing a critical layer of insight: kinetics. Terry Kenakin’s latest lecture in Terry’s Corner  delivers exactly what your discovery teams need now: a pragmatic framework to interpret kinetic binding experiments and recognize when a drug’s rate of onset and offset matter more than affinity itself. Prevent wasted cycles:  Avoid costly delays caused by false positives from static affinity readouts. Gain operational clarity:  Learn how kinetics signal which compounds will truly perform in vivo—under competitive, real-world conditions. Stay ahead of competitors:  Know when your data reflects equilibrium and when to probe deeper, ensuring your team doesn’t misinterpret key signals. Premium Members get 50%+ discount when they join Terry’s Corner. 🔒 Available only in Terry’s Corner - Premium Members get an exclusive discount Sharpen your discovery decision ➤ 🗣️ “Dr. Kenakin is a masterful teacher and communicator—and a leading expert in our field.” — Dr. GPCR University Course Attendee Dr. GPCR Podcast : From Personal Pain to Scientific Purpose: Alex Serafini’s Journey We sit down with Dr. Alex Serafini, whose unconventional path—from patient to scientist—exemplifies why personal mission matters in translational research. Serafini’s early struggles with chronic pain sparked a career focused on innovating where pain management has long stagnated. His work challenges outdated targets, explores overlooked roles of GPCRs and RGS proteins in pain, and seeks to redefine translational models for patient realities. Redefine your playbook:  Why Serafini believes that pain research needs to start from clinical phenotype and work backward. Explore blind spots:  The underestimated role of GPCRs and RGS proteins in chronic pain mechanisms. Rethink translational success:  How post-COVID insights and unconventional decision-making shaped Serafini’s high-impact projects. Watch the conversation ➤ Event: Where the Next Decade of GPCR Therapies Will Be Defined The 20th annual Discovery on Target GPCR-Based Drug Discovery  meeting is where the next wave of therapies—from allosteric modulators to computational targeting—will take shape. If you’re not there, you’re missing an opportunity to benchmark your strategy against the best in the field. Terry Kenakin’s featured talk on “The Kinetics of Allostery” offers a rare live glimpse into advanced kinetic thinking—but for full, actionable frameworks, only Terry’s Corner  members get exclusive on-demand access. Benchmark your roadmap:  See where competitors are heading before they act. Identify emerging targets:  Allosteric modulators, biased ligands, and kinetic frameworks will dominate the next wave. Get exclusive discounts:  Secure your seat now with code DRGPCR25 for $200 off. Secure your spot ➤ Why Dr. GPCR Premium Membership Gives You an Edge Premium delivers curated, noise-free intelligence every week: deep-dive expert lectures, classified industry news, priority event alerts, job opportunities, and insider commentary—all designed to help you move faster and smarter in an increasingly complex GPCR landscape. Stay focused, informed, and ahead of your competitors while saving critical time each week. Dr. GPCR Premium is designed for scientists who need the right intelligence, fast—without noise, distractions, or delays. Every week, members get: A full edition of GPCR Weekly News : jobs, events, papers, industry updates Exclusive discounts on Terry’s Corner  digital pharmacology courses Priority access to insights from major conferences, emerging research, and expert commentary Whether you’re a pharmacologist, biotech scientist, or team leader, Dr. GPCR Premium gives you an edge in a fast-moving field. 🔹 Premium Membership FAQ 🔹 What’s included? The complete Weekly News digest, curated jobs, upcoming events, classified GPCR publications, exclusive on-demand expert frameworks, and member-only discounts. 🔹 Who is it for? GPCR scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who need fast, curated, career-relevant intelligence to stay ahead. 🔹 Why now? The pace of GPCR innovation is accelerating. Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won’t see coming. Don’t Fall Behind—Access the Edge You Need 👉 Ready to sharpen your discovery decisions? Join today and get instant access to exclusive insights, expert frameworks, and classified intelligence that give you a professional edge: Premium Signup Already a Premium Member? Access this week’s full Premium Edition here ➤    Access all the news and upcoming events Hashtags: #GPCR #DrGPCR #BindingAffinity #Pharmacology #DrugDiscovery #LeadOptimization #TerryKenakin #EmergingDrugHunter #EfficientDiscovery #PipelineAcceleration

Watch Episode 170 Why We’re Here What if your own body pushed you into science? For Dr. Alex Serafini, that’s exactly what happened. After years of living with unresolved pain following surgery for a pilonidal cyst, Alex was left without options — and without relief. Denied stronger medication in the midst of the opioid crisis, he turned to the one place that still offered answers: the lab. This is a story about how chronic pain doesn't just shape lives — it reshapes careers. From Patient to Researcher Alex wasn’t always planning to be a scientist. Born in California and raised in Silicon Valley, his early interests were in finance and business. But everything changed when his recurring pain — and the rigid protocols around opioid prescription — forced him to search deeper. “I wasn’t able to get stronger pain meds,” he said. “So I had to understand the biology myself.” His new obsession led him to Johns Hopkins, where he worked in the lab of Dr. Mike Caterina on pain mechanisms in the peripheral nervous system. There, he learned how to frame pain not just as a symptom, but as a signal — and a scientific challenge. The Value of Lived Experience in Science What makes Serafini’s trajectory so compelling isn’t just his technical training — it’s the urgency he brings to the field. His interest in model development, in capturing the lived human experience through preclinical systems, was born out of necessity. Building a Career from the Inside Out Now back in med school, Serafini aims to follow the physician-scientist path: part-time clinical work, mostly lab-based research. He’s focused on RGS proteins , pain comorbidities  like addiction and depression, and pushing for more accurate model systems. "When you talk to patients that have an unmet need, you learn things that no one is thinking about in terms of how to solve those problems." Takeaway Science isn’t always about curiosity. Sometimes, it’s about necessity. Dr. Alex Serafini’s journey proves how personal pain can lead to professional purpose — and why the next generation of pain researchers needs to start from lived experience, not just literature. _________________ Keyword Cloud: GPCR research community , chronic pain , GPCR drug discovery , GPCR scientist network , pain neuroscience

Think a drug just "locks into" a receptor and does its job? Think again. Join Terry Kenakin as he pulls back the curtain on the deceptively simple process of orthosteric binding—the first step in drug action. This isn’t just about molecules finding a pocket. It’s about a dynamic dance of chemical forces, equilibrium shifts, and molecular decisions that determine whether a compound works… or doesn’t. The Importance of Binding in Drug Action In pharmacology, binding must happen before any drug effect can take place. Understanding this process is crucial for anyone interested in drug development and action. When a drug binds to its target, it initiates a series of events that can lead to a physiological response. This foundational knowledge guides researchers in the development of new therapeutics. Key Concepts in Binding Terry unpacks several key concepts related to orthosteric binding: Langmuir Adsorption Isotherm : This concept teaches us about affinity. It explains how the concentration of a drug influences its binding to the receptor. A high affinity means the drug will bind more easily and effectively. Binding Curves : These curves reveal presence, not potency. They show how much of a drug is binding to its target but do not necessarily indicate how strong its effect will be. Understanding EC50 : The term EC50 refers to the concentration of a drug required to achieve 50% of its maximum effect. However, this doesn’t always mean what you think it means. Often, a low EC50 indicates high potency, but this isn't always the case due to various biological factors. 📚 Whether you're new to pharmacology or brushing up on basics, this lesson will change how you think about the very first interaction between drug and target. Unlocking the Secrets of Orthosteric Binding Understanding why some drugs bind better than others is crucial for drug efficacy. It can inform decisions in drug design, improving therapeutic outcomes and reducing unwanted side effects. 🔥 Want to understand why some drugs bind better—and why that matters? The Dynamic Nature of Binding Binding is not a static event. Instead, it involves a dynamic interaction between the drug and the receptor. The receptor may change shape upon binding, affecting how the drug interacts and how effective it will be. Additionally, competitive inhibitors can interfere with this binding process, leading to reduced efficacy. Implications for Drug Development As drug developers, understanding these nuances can significantly impact the success of new medications. By considering factors like the Langmuir adsorption isotherm and binding curves, researchers can better predict how a drug will perform in the body. This knowledge can guide modifications to improve binding affinity and bioavailability. Conclusion In conclusion, the process of orthosteric binding is complex and multifaceted. It goes beyond simple interactions. The dynamic interplay of chemical forces shapes drug effectiveness. Unlock "Orthosteric Binding" now and dive deeper into this fascinating topic. You'll gain valuable insights into the critical role binding plays in pharmacology. This understanding can enhance your appreciation for drug development and therapeutic action. By embracing these concepts, we can pave the way for more effective treatments in the future. Understanding the intricate details of drug-receptor interactions transforms how we approach pharmacology.

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 pace it should. I've seen this pattern unfold across biotech, academia, and nonprofits. The assays are running, data is flowing in from your CROs or your internal labs , yet progress stalls. Decisions are slow, crucial data is siloed, and despite everyone working hard, programs drift. For over two decades, my work has centered on GPCR pharmacology . In every role and sector, I found myself drawn to the same critical challenges: missed opportunities, misaligned systems, and promising programs stalling despite strong science. I was always the one identifying what could be improved: The essential structure that was missing. The clarity that was desperately lacking. The unnecessary friction that slowed everything down. Traditional roles rarely gave me the freedom to implement these changes at the scale needed. So, I created a new path—one that allows me to embed, optimize, and accelerate GPCR programs from the inside out. The GPCR Data Dilemma: The Lego Bucket Problem I've seen promising GPCR programs generate massive volumes of high-quality data. But without structure, it's just a messy pile of colored blocks. I call this the Lego Bucket Problem . You have the data, but not the definitive direction. This disconnect frequently leads to: Underperforming assays. Internal data and CRO outputs  misaligned with strategic goals. Delays in critical go/no-go decisions. Frustrated teams and slipping timelines. It's not just a scientific issue—it's an operational one. You can't move fast without clarity, and you can't make confident decisions without robust structure. My Approach: Biology, Execution, Systems My consulting approach uniquely blends deep pharmacology expertise with the operational discipline required to make that expertise actionable. Here's how I bring a fresh perspective: Biology-First, Data-Driven Strategy:  I help you focus on the science that truly matters. We cut through the noise, elevate what's working, and strategically solve what's not, ensuring your GPCR program stays on target. Embedded Execution:  I work alongside your team—not above it. I'll help write CRO scopes, meticulously review assay data, flag risks early, and keep your programs relentlessly on track. Systems That Drive Progress:  From assay tracking to data workflows, I design simple, scalable tools that surface insights early and dramatically reduce delays, transforming your data into actionable intelligence. A Broader Lens: Dr. GPCR As the co-founder of Dr. GPCR, we've built a global hub connecting over 1,300 GPCR scientists dedicated to this field. These ongoing conversations keep me on the front lines, sharpening my understanding of the common bottlenecks and evolving needs across the entire GPCR community. My Consulting Philosophy This practice is built on three core values: Scientific Integrity:  Every recommendation is grounded in real-world evidence and extensive experience. Operational Discipline:  Robust systems and clear structure aren't "nice to have"—they are absolutely essential for efficient progress. Collaborative Partnership:  I embed, contribute, and build solutions hand-in-hand with your team. Ready to Move Your GPCR Program Forward? If you're navigating a stuck GPCR program, planning your next crucial milestone, or struggling to gain clarity from complex data, I'd love to help. 📌 Learn more about my services: Yamina.org 📅 Book a 30-minute strategy call: https://calendly.com/drgpcr/yamina-corner

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 because the data becomes a mess. I call it the Lego Bucket Problem : You’ve got CRO output, internal assay data, maybe even some promising signals. But there’s no blueprint. No structure. No clear path to your next milestone. Meetings drag. Decisions stall. And momentum quietly dies. The Hidden Cost of Good Science Without Systems I’ve seen this pattern again and again—across academia, biotech, and through close work with dozens of teams inside the Dr. GPCR Ecosystem. Strong science. Promising data. But no systems to turn it into momentum. Data arrives too fast and too fragmented CROs deliver output without clear integration Teams chase the wrong assays, too late to pivot Milestones slip—and nobody realizes until it’s too late Failing fast? Not possible when nothing’s built to surface the right  insights early. That’s Why I Built Yamina’s Consulting Corner This is not “advising.” This is embedded consulting for biotech and VC teams who need to move fast —without compromising scientific integrity. Unlike traditional advisors, I'm not just observing; I'm part of your team . This allows me to experience your challenges firsthand, identify roadblocks faster , and i mplement solutions from within , ensuring genuine buy-in and lasting momentum. Here’s what I bring: Biology-First Strategy I’ve designed GPCR assays, led collaborations across research environments, and translated complex data into action. I know how to ask the right scientific questions—and when to shift from analysis to execution. Systems That Drive Execution No more disconnected slides and 6-week meeting cycles. I install simple tools that surface insights, align your team, and keep momentum moving. True Embedded Partnership I review CRO scopes, flag risks early, and sit in on your strategic calls. I’m not watching from the sidelines—I’m driving with you. Real-Time Global Insight As founder of Dr. GPCR, I’m connected to 1,300+ scientists and decision-makers worldwide. That network gives me a constant pulse on what’s working—and what’s next. Who I Work With ✅ Biotech Teams  – Especially those lacking in-house GPCR leads or overwhelmed by CRO data chaos. ✅ Venture Capital Firms  – Looking to accelerate, troubleshoot, or validate GPCR assets in their portfolio. ✅ Contract Research Organizations (CROs)  – Wanting to better align with biotech clients and deliver real  insight, not just data. My Consulting Philosophy Every successful GPCR program is a blend of scientific excellence  and operational precision . One without the other will quietly kill your momentum. My work is rooted in: ✔️ Scientific Integrity ✔️ Operational Discipline ✔️ Collaborative Partnership Let’s Get Your GPCR Program Moving Again Whether you’re building from scratch or recovering from a stall, I’ll help you move faster—with fewer blind spots, tighter execution, and a clear line of sight to your next key decision. 🚀 Book your free 30-minute strategy call Let’s unlock the momentum your GPCR program needs. 👉 https://calendly.com/drgpcr/yamina-corner Or explore how we can work together: 👉 Yamina.org 🔑 Key Takeaways ✅ Even strong science stalls without operational structure ✅ Scattered data = missed insights = wasted time ✅ You can’t fail fas t if you can’t see the problems early ✅ Most teams don’t need more data— they need clarity ✅ Yamina’s Corner helps teams move from data chaos to decisive action ✅ This is hands-on support —not passive advising p.s: Still unsure if this is the right fit? Let’s talk through your program—no pitch, just clarity.

Watch here Trends come and go. Scientific fads rise and fall. But Sokhom Pin stayed loyal to GPCRs , even when big pharma turned its gaze to other targets like kinases and checkpoint inhibitors. Riding the GPCR Rollercoaster Early in his career at DuPont and BMS, GPCRs were red hot. High-throughput screening for receptor ligands was booming, and Sokhom was at the center of it. But then came the industry shift. “Companies started shutting down neuroscience and GPCR programs. But I stayed,” Sokhom said. While others pivoted, Sokhom went deeper: refining assays, exploring signaling bias, and building a robust knowledge base in one of the most pharmacologically diverse receptor families. The Payoff of Staying Focused Today, GPCRs are making a comeback in popularity. Advances in biased signaling, allosterism, and endosomal signaling have opened new therapeutic frontiers. And Sokhom? He’s one of the few who never left. “Because the field became unpopular for a while, they stopped training new experts. Now, there’s less competition and more opportunity.” A Career Built on Consistency From CGRP receptor antagonists at BMS to opioid receptor research at Alkermes and early-stage work at Cerevel and Superluminal, Sokhom’s consistency has paid off in ways short-term thinkers often miss. _______________ Keyword Cloud: GPCR drug discovery , G protein-coupled receptors , GPCR webinar series , GPCR scientist network , GPCR research community

Watch Episode 169 Leadership in science isn't just about results, it's about people. At Alkermes , Sokhom Pin wasn’t just leading GPCR programs; he was building culture from the ground up. And that culture worked. The Challenge: Build a Team. Build a Lab. Build the R in R&D. When Sokhom joined Alkermes, the company had a strong development arm, but a relatively underdeveloped research function. He was tasked with building an in vitro pharmacology group from scratch , including infrastructure, hiring, assay development, and team dynamics. “I couldn’t sleep. I was up every night thinking about how to hire, how to lead, how to avoid the mistakes my bad bosses made,” Sokhom said. What Made It Work He focused on empowerment , not micromanagement He hired based on attitude and team fit , not just credentials He designed lab workflows that encouraged curiosity without burnout He supported work-life balance while maintaining scientific excellence The result? His team was known internally as the “happiest group at Alkermes.” Why Culture Matters in Drug Discovery You can’t innovate under pressure. In a field like GPCR research (where data complexity and failure rates are high), scientific rigor thrives when trust and collaboration lead the way. Sokhom knew this instinctively and built a system to support it. From Lab Bench to Boardroom His work at Alkermes didn’t just improve drug screening outcomes, it redefined what great leadership in biotech looks like . It was the foundation for his next opportunity: helping launch Cerevel from the ground up. ________________ Keyword Cloud: Dr. GPCR ecosystem , GPCR research community , GPCR podcast , GPCR data platform , GPCR training program

Watch Episode 169 What if you could earn a PhD while supporting a family and working full time in drug discovery? That’s exactly what Sokhom Pin did. In a field where traditional academic paths often dominate the narrative, his story offers a powerful alternative. Breaking the Mold Most scientists follow the usual script—graduate school, lab rotations, dissertation defense. But Sokhom’s journey started differently. As a lab technician at Johns Hopkins, he was fascinated by science but also grounded in real-life responsibilities. With a growing family and a full-time position, traditional PhD training just wasn’t an option. Instead of choosing between academia and career, he engineered a third path : a partnership between BMS and UConn that allowed him to do industry-based research while pursuing his doctorate. “I couldn’t afford to quit my job. So I designed my own PhD program,” Sokhom shared. How It Worked BMS funded the research, salary, and even tuition UConn accepted the research done in the BMS lab as part of the dissertation Sokhom met weekly with advisors and monthly for presentations All research was publication-quality, high-impact, and strategically focused This approach allowed him to avoid the experimental churn common in academia. He only pursued experiments that were scientifically sound and directly publishable, a skill honed from years of hands-on work in high-throughput screening. A Model for Future Scientists? Sokhom’s experience speaks to a larger truth: there’s no single way to become a scientist . His hybrid path is a model of possibility for professionals in the biotech industry who still dream of earning advanced degrees without leaving the bench, or their paycheck, behind. Takeaway If you’re navigating work, life, and scientific ambition, Sokhom Pin proves it’s possible to have it all, if you design it yourself. _________________ Keyword Cloud: GPCR training program , GPCR scientist network , GPCR drug discovery , G protein-coupled receptors , GPCR online course

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 lessons by Dr. Terry Kenakin with short videos, clear summaries, and curated references. New and unique lessons are released weekly on Tuesday. Elevate your drug discovery program with 45+ lessons yearly. Premium Members:  Get your exclusive discount code in this week’s full edition of the this newsletter accessible at the bottom of this email.   Join Terry’s Corner Today Yamina’s Corner Is Live – Are you drowning in disorganized data? Yamina’s Corner delivers GPCR consulting that cuts through the noise, designing assay cascades, setting go/no-go points, and de-risking programs from hit validation through development candidate selection and beyond. With a biology-first strategy, embedded execution, and scalable systems, it turns scattered data into decisions, accelerating your path to a successful preclinical program. Because even the best data means nothing without structure. That’s the Lego Bucket Problem.    Visit Yamina’s Corner Now CELT-335 - Celtarys Validates New Assay for CB1/CB2 Screening Dr. GPCR partner Celtarys Research has validated a TR-FRET assay for cannabinoid receptor ligands using their probe CELT-335. With nanomolar affinity, high specificity, and a strong signal-to-noise profile, this non-radioactive, cell-compatible platform is ready for your next SAR-driven screening campaign.   Read The Full Article GPCR Publication Highlights   Chemokine–GPCR Selectivity Unveiled Sequence- and structure-based analysis reveals how conserved and variable regions across chemokines and their receptors drive selectivity and promiscuity, paving the way for rational ligand design.   Decoding PTH1R Gq Signaling Cryo-EM structures of Gq-bound PTH1R uncover glycan and loop-based mechanisms shaping G-protein preference, offering a path toward signaling-biased osteoporosis therapies.   Distinct Ligand Activation in NMBR Simulations show how two ligands differently activate class A GPCR NMBR, with allosteric communication hubs modulating signaling, advancing antipruritic drug strategies. Want the full breakdown and your discount code for Terry's Corner? Better pharmacology leads to better decisions—unlock it now with Terry’s Corner. Stay curious,   The Dr. GPCR Team Join Our Newsletter! To start receiving our newsletter in your inbox every Thursday, follow these simple steps: Select the Log In / Sign Up option located at the top right corner of the header. Select ' New to this site? Sign Up' Complete the registration form. Stay updated with the latest news and insights by signing up today!

Picture this: two compounds bind to the same receptor. One sparks a firestorm of cellular activity. The other? Silence. Why? The answer lies in a misunderstood property called efficacy—the power of a drug to trigger a response after  binding. In Terry Kenakin’s latest lesson, you’ll uncover why efficacy is the unsung hero of drug discovery and how its effects depend entirely on the biological system it’s tested in. This isn’t just a theory class. Terry walks you through real-world experiments, decades of receptor pharmacology wisdom, and the cutting-edge operational model used to quantify efficacy. You'll learn why some agonists succeed in sensitive tissues but fail elsewhere—and how this knowledge can dramatically shift your screening strategy. If you’re stuck trying to figure out why your lead compound looks promising in vitro but flops in vivo, you need this lesson. Ready to think beyond binding? 🔓 Find the lesson in Terry’s Pharmacology Vault: “Efficacy and System Sensitivity Unlock "Agonism & Efficacy" now

What do roasted ox liver and AI-powered virtual screening have in common? They both mark critical moments in humanity’s centuries-long quest to control physiology—and they bookend a story few new learners truly understand. In this exclusive foundational-level lecture, Dr. Terry Kenakin takes you on a captivating tour through the history of pharmacology : a journey that spans ancient Egypt, revolutionary scientific ideas, Nobel Prize-winning discoveries, and today's digital frontier. But this isn't just about what was —it's about why the past matters now. Ever heard of the Ebers Papyrus? It’s one of the earliest medical texts, prescribing liver to treat night blindness. (Spoiler: It worked—thanks to Vitamin A.) Fast-forward a few thousand years, and we’re talking beta receptors, receptor theory, and AI-generated ligands. All of it connected. All of it is essential. Dr. Kenakin also celebrates the giants on whose shoulders we stand—A.J. Clark, Paul Ehrlich, Sir James Black, and more—sharing the stories and setbacks that shaped today’s scientific frameworks. And yes, you'll even meet the man who turned failed experiments into a Nobel Prize-winning discovery about nitric oxide. Whether you're stepping into pharmacology for the first time or rekindling your interest, this lesson delivers 'aha' moments  grounded in decades of experience. It's equal parts inspiration, insight, and orientation. Curious yet? 👉 Join Terry’s Corner, your essential launchpad into the world of therapeutic science Unlock "The History of Pharmacology" now

What if one simple graph could reveal the true power of a drug? In the newest foundational lesson from Terry Kenakin’s Pharmacology Vault , we unlock the visual language of pharmacology: dose-response curves . From assessing drug potency to predicting effects, these curves aren't just for data—they’re your entry point to understanding drug behavior at a deeper level. In classic Terry style, the lecture walks you through: What dose-response curves are and why they’re indispensable How curve-fitting models can  deceive—and how to avoid being misled The statistical tricks that elevate a rough curve into a real insight You'll leave with practical tools and a new appreciation for the humble curve that powers drug discovery. Want to finally understand EC50 without squinting at formulas? Ready to grasp how a curve can mislead—or enlighten? 👉 Discover why dose-response curves are the backbone of all pharmacology. Unlock "Dose-Response Curves" now

What if the way we've been studying GPCRs—arguably the most important drug targets in pharmacology—has been wrong… or at least, incomplete? In the foundational lesson of Terry’s Corner , Dr. Terry Kenakin invites us to challenge outdated assumptions and step into a new era of drug discovery. With insights from molecular dynamics, biased signaling, and allosteric modulation, this session lays bare the science that’s reshaping how we develop medicines. Here’s the surprising truth: up to 80% of GPCR-targeted drugs fail—not because of poor chemistry, but because we’ve misunderstood how these shape-shifting proteins truly behave. Now, Terry is opening the vault. This isn’t theory. It’s 40 years of hard-won insight distilled into accessible, high-impact content designed for learners just starting out. This is your chance to get ahead of the curve. Join Terry’s Corner and stay updated on the latest in GPCR research—delivered in a format that’s as approachable as it is transformative. 👉 Ready to understand what your molecules are really doing? Unlock "Why Terry's Corner" now

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 semaglutide’s Canadian patent expiry is opening competitive pathways. Eli Lilly’s next moves with Orforglipron and its amylin analog are highly anticipated.   Plus, Celtarys explores ligand selection for better assays, and co-founder Dr. Maria Majellaro shares her story of innovation and listening-driven science.   This week’s publication highlights: CXCR4 takes on a nuclear role in red blood cell maturation CXCL13/CXCR5 emerges as a high-potential pain target ST171, a biased 5‑HT1A agonist, delivers selective pain relief in preclinical models Dr.GPCR Updates Terry’s Corner  – Build Better GPCR Screens with Dr. Kenakin   Four decades of receptor theory now fit in one expert-guided hub. Terry’s Corner gives you timeless and timely tools to improve selectivity, model efficacy, and design smarter GPCR pharmacology screens, anchored in real-world lessons and cutting-edge science.   Sign Up for The Kenakin Brief Fluorescent Ligands vs. Radioligands – Assay Smarter Celtarys explores how fluorescent ligands enable safer, high-throughput screening with rich kinetic data. Learn how these tools help retain assay integrity while eliminating radioactivity—perfect for next-gen GPCR workflows.    Upgrade Your Screening Strategy Leadership in Ligand Design  – The Celtarys Origin Story   In  this founder interview , Dr. Maria Majellaro reveals how Celtarys evolved from a vision into a company solving real-world assay problems. It’s a story of leadership, scientific rigor, and tools built for the needs of modern discovery teams.   Read Maria’s Story GPCR Publication Highlights   CXCR4 signaling promotes terminal erythropoiesis  through nuclear translocation and perinuclear calcium bursts.  Blocking this chemokine axis reduces pain  hypersensitivity by dampening neuroinflammation and glial activation.  This novel agonist activates Gi/o selectively , avoiding β-arrestin and showing strong pain relief in preclinical models. Want the full breakdown? Explore this week’s research, tools, and biotech insights in one place. Stay curious, stay connected, because the future of GPCR science is being written pathway by pathway.   Best,   The Dr. GPCR Team

Ever wondered why a drug behaves like a miracle in one tissue and a dud in another? Welcome to Terry’s Corner , where foundational pharmacology is demystified by someone who’s spent over 40 years navigating the complexity of drug discovery. In his newest lesson, “The Uniqueness of Pharmacology in Drug Discovery,” Terry Kenakin explains why pharmacology isn’t a clean-cut science—it’s a dynamic dialogue between molecule and system. You’ll uncover: Why pharmacology is the glue between chemistry and biology How to interpret drug behavior across tissues The truth behind those “confusing” lab results that seem contradictory This lesson isn’t just academic—it’s practical knowledge every early-stage scientist needs. Whether you're heading into your first assay or trying to make sense of inconsistent data, Terry gives you the tools and mindset to understand what's really  happening. Don’t just look at the data—learn how to read the story it’s telling. 👉 Start your journey with Terry’s foundational series Unlock "Unique Role of Pharmacology" now

What happens between identifying a target and delivering a life-saving treatment? How do molecules make the leap from laboratory concept to therapeutic reality? Step into the world of drug discovery with Dr. Terry Kenakin , a veteran pharmacologist with over 40 years of industry experience. In this foundational-level  lesson, Terry unpacks the real-life process behind discovering new drugs, breaking down the science into accessible, engaging insights for early learners and curious minds. You’ll explore: What makes a “discovery team” tick (and why teamwork is non-negotiable) The difference between Me Too  and First in Class  projects—and why both are essential Why target-based  discovery is powerful, but can miss the forest for the trees The critical importance of translation —turning lab data into meaningful therapeutic outcomes Terry’s unique ability to combine storytelling, real-world experience, and scientific clarity makes this more than just a lecture—it’s a launchpad. If you're just beginning your pharmacology journey… This is the lesson that will connect the dots. You’ll leave with the language, logic, and big-picture view that underpins all future learning in pharmacology and drug development. Don’t miss your chance to learn from one of the best: Unlock “Introduction to Drug Discovery" now

Watch Episode 168 In drug discovery, tools matter, but so do people. In Episode 168 of the Dr. GPCR Podcast, Dr. Maria Majellaro makes it clear that Celtarys isn’t just a ligand provider. It’s a scientific partner. And that mindset is precisely what makes their new partnership with Dr. GPCR so powerful. “We don’t just deliver compounds, we solve assay problems.” — Dr. Maria Majellaro Celtarys specializes in the custom development of fluorescent ligands  using a modular chemistry platform. Their method allows researchers to explore different linker positions, tailor activity (agonist or antagonist), and retain biological function, all while skipping the time-consuming synthetic routes common in the field. But what sets them apart isn’t just chemistry. It’s empathy. Maria emphasizes the importance of genuinely listening to researchers: understanding the biological question first, then building a tool to match it. Whether supporting CROs, academic labs, or pharma teams, Celtarys engages deeply with collaborators to deliver not just reagents but solutions. “We want to illuminate biology. That’s the mission. ” — Dr. Maria Majellaro Now, as official partners of the Dr. GPCR ecosystem , Celtarys is opening up that model to the broader research community. The goal? Democratize access to high-performance chemical probes and make assay development faster, cheaper, and more customizable. 👉 See how Celtarys can support your drug discovery workflow on the company page . _______________ Keyword Cloud:   GPCR data platform , fluorescent ligands , assay development , GPCR research community , Dr. GPCR ecosystem , GPCR webinar series

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 the know. Celtarys Research expands its assay tools with CELT-419 for D3 receptor studies, and Dr. Maria Majellaro shares her journey to founding Celtarys in "From Lab to Leadership". Explore her path from postdoc to platform builder.   Also this week:  – Phosphorylation’s selective role in β-arrestin recruitment across class B1 GPCRs  – GPCR mutations in cancer—drivers, passengers, or both?  – CXCR4 oligomer disruption boosts therapeutic response in lymphoid neoplasms Dr. GPCR Updates Learn Pharmacology That Drives Discovery  – From Dr. Terry Kenakin   Terry’s Corner is your space focused on GPCR pharmacology designed just for you.  Dr. Terry Kenakin brings translational clarity to complex receptor concepts.   This is more than review, it’s readiness. Learn binding, bias, kinetics, and core models—fundamentals that fuel confidence and fluency Move beyond theory to apply selectivity, ADME, and early safety in real development contexts Advance with nuanced lessons on allostery, residence time, and translational PK/PD   Subscribe to The Kenakin Brief Fluorescent Probe CELT-419 Powers D3R Binding Assays Across Platforms   Celtarys Research presents CELT-419, a nanomolar-affinity fluorescent ligand optimized for D3 receptor assays in both baculovirus and live-cell systems. With strong signal stability, HTS compatibility, and broad assay versatility, CELT-419 is designed for deeper kinetic, competitive, and equilibrium binding insights.    Explore Dr. GPCR Partner Tools The Story Behind Celtarys – From Chemistry to Company   How does a medicinal chemist become a biotech founder? This blog post breaks down Dr. Maria Majellaro’s path from lab research to co-founding Celtarys, as told in her recent Dr. GPCR Podcast appearance. Read how scientific need and timing drove the leap from academia to application.   Read the Story GPCR Publication Highlights     Phosphorylation selectively regulates β-arrestin recruitment  across glucagon family receptors, revealing that GLP-1R and GIPR rely on phosphorylation while GCGR does not.  GPCR mutations in cancer   show both driver-like patterns and high redundancy, prompting a call for multiomics to distinguish signal from noise.  CXCR4 oligomerization  sustains oncogenic signaling in lymphoid neoplasms, and its disruption boosts sensitivity to the apoptosis-inducing drug venetoclax. Want the full breakdown? Explore this week’s research, tools, and biotech insights in one place. Keep pushing the boundaries, because your work moves molecules and medicine forward.    Stay curious,   The Dr. GPCR Team

Watch Episode 168 Success in science is rarely linear. It’s a mosaic of risks, setbacks, and tiny wins that lead to clarity. Dr. Maria Majellaro’s story, shared in Episode 168 of the Dr. GPCR Podcast, is filled with such moments, from bombing her first high school chemistry test to co-founding a startup delivering tools for GPCR drug discovery. “The first time I wore my lucky cactus shirt to a major meeting... and it led to a game-changing collaboration.” — Dr. Maria Majellaro Maria didn’t always know she’d end up in a startup. In fact, her early decisions were based on curiosity, instinct, and a surprising love of cooking (yes, she even compares molecule design to perfecting focaccia). She studied pharmacy with a specialization in pharmaceutical chemistry, a degree that allowed her to see the full picture from synthesis to biology to formulation . Her turning points? Getting accepted into a PhD program during a personally difficult time. Saying yes to a postdoc opportunity abroad. Choosing not to overthink major career decisions, because as she puts it:  “A lot of friends of mine told me also, you already know what you want to do.” — Dr. Maria Majellaro Now, she leads a team of talented chemists at Celtarys, developing fluorescent ligands that help drug discovery teams better understand GPCR function. With the new  Dr. GPCR x Celtarys partnership , she’s extending those insights to researchers worldwide. 👉 Explore Celtarys’ tools and partnership with Dr. GPCR on the company page . _______________ Keyword Cloud:   GPCR scientist network , career development , fluorescent ligands , GPCR training program , Dr. GPCR ecosystem , GPCR podcast