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A Result That Looks Clean but Isn't That interpretation may be wrong. Not because the assay failed technically, but because of what steady-state measurement structurally cannot reveal when two opposing activities are present in the same scaffold. This is the kinetic detection problem in multi-target GPCR activity, and it has consequences for how scaffolds are interpreted at early stages of discovery. What This Article Does Not Cover From This Week's Lesson The kinetic detection argument is one piece of the lesson. The lesson also works through: Why certain disease architectures require multi-target engagement in the first place, and the therapeutic contexts where single-receptor pharmacology is a precision mismatch Hybrid ligand design: how two pharmacophores are encoded into one scaffold, and why a uniform PK profile changes what co-administration cannot achieve How amino acid substitution within incretin peptide sequences shifts receptor selectivity across GLP-1, GIP, and glucagon receptor types The two-edged character of multi-target engagement: why therapeutic breadth and side effect liability advance together The detection problem examined in this article is the final piece. It is also the one most consequential for how multi-target compounds are evaluated once they exist. The Steady-State Cancellation Problem A scaffold carrying both agonist and antagonist activity presents a detection problem that standard assays are not designed to resolve. At steady state, the assay captures the net effect of whatever the compound is doing at equilibrium. If the agonist activity and the antagonist activity in the scaffold are roughly balanced, the net effect approaches zero. The readout is flat. The compound appears inert. Nothing in the steady-state result signals that two active processes are cancelling each other. The data is not incorrect. It is incomplete in a way the assay cannot disclose by design. Dynorphin A is a case that makes this concrete. The peptide sequence carries a region responsible for efficacy and a separate region that functions as a binding address. If a fragment loses the efficacy-bearing portion, what remains is an antagonist. In a preparation containing both the full agonist and the antagonist fragment, steady-state observation would reveal only a progressive reduction in response as the ratio of antagonist increases. The underlying dual activity remains invisible. What Kinetics Surfaces Agonist and antagonist activity do not proceed at the same rate. Onset kinetics differ. And those differences, invisible at equilibrium, become visible in real-time observation. When a scaffold carries both activities, kinetic assays produce complex time-dependent response curves. An initial agonist response emerges first. Then the antagonist effect, developing at a different rate, begins to modify it. The curve shape is not noise. It is a pharmacological signature of two processes with different temporal profiles. Dr. Kenakin describes this in the session: "You will see these complex curves. You see agonism, but then you'd start to see the other effect kick in. Kinetically, however, you might see it." Ambenonium demonstrates this with unusual clarity. The compound is simultaneously a muscarinic receptor inhibitor and a cholinesterase inhibitor, two activities that oppose each other functionally. At steady state, the effects cancel, and the compound appears to have no net action. In real-time observation, both activities emerge as distinct, time-separated signatures: one potentiating acetylcholine through cholinesterase inhibition, the other attenuating the response through receptor blockade. The compound is not inactive. It is pharmacologically complex in a way that steady-state measurement assigns no value to. What This Means for Multi-Target Programs The implication is practical. A scaffold that reads as inactive under standard screening conditions may carry multiple activities that are cancelling at equilibrium. Dismissing it on the basis of that result forecloses something that kinetic investigation might recover. The broader point is a methodological one. Steady-state assays answer the question they are designed to answer: what is the net effect at equilibrium? They are not designed to disaggregate that net effect into its components. When a multi-target scaffold is the subject of investigation, the question being asked and the information the assay returns may not match. Kinetic approaches reframe the question. Rather than asking what the compound's net effect is, they ask how the compound's effects develop over time. That reframing is what makes the underlying pharmacological complexity visible. Why Terry's Corner The kinetic detection argument is one piece of what the session covers. The lesson develops the surrounding framework: why certain disease architectures require multi-target engagement in the first place, the design strategies for building it into a single scaffold, and how peptide sequence modification shifts receptor selectivity in predictable directions. The detection problem examined here is the final piece, and the one most consequential for how multi-target compounds are evaluated once they exist. Terry's Corner is the room where pharmacologists work through frameworks like these alongside Dr. Terry Kenakin. Structured lessons are the foundation. Live AMAs and workshops are where the thinking comes alive, and where the question you've been sitting on finally has somewhere to go. 🟢 40 years of expertise at your fingertips: Explore the complete library ➤ ✳️ Want to know what's inside? Read the latest articles ➤ Stay sharp between lectures. Subscribe to The Kenakin Brief today ➤ Follow the thinking. Terry's Corner on LinkedIn ➤ Check out the YouTube Channel. Terry's Corner on YouTube ➤

A Specific Difficulty, Not a General Verdict A pharmacologist designing an orthosteric small-molecule agonist for a family B GPCR encounters a pattern that recurs often enough to deserve a structural explanation. The molecule binds. The affinity is reasonable. The activation is weaker than the receptor's natural peptide agonist suggests it should be. The pattern is not universal, and it does not mean the orthosteric site is undruggable. It does mean that stabilizing the receptor's active state through a small molecule, at this specific class of GPCRs, is harder than orthosteric small-molecule programs at smaller receptors have led the field to expect. The reason has a structural account. It is one model among several, but it explains the observation cleanly, and it has practical consequences for how programs at peptide receptors approach modality choice. What GPCR Biologic Drugs Reveal About the Active-State Problem Family B GPCRs are conformationally malleable. The receptor samples many states. To produce agonism, a ligand must do more than occupy the binding pocket. It must stabilize the active conformation specifically, long enough for downstream signaling to proceed. GPCR biologic drugs, peptides in particular, achieve this through a mechanism worth naming carefully. A peptide agonist makes contact with the receptor across numerous regions of the binding site. Each contact contributes modestly. Together, they form what receptor pharmacologists describe as affinity traps: distributed networks of interactions that hold the receptor in an active state by satisfying many constraints at once. The active state is, on this account, the conformation in which the largest number of those contacts are simultaneously engaged. The peptide does not pull the receptor into activation. It selects for it, through the geometry of where its contacts can reach. Why an Orthosteric Small Molecule Has a Harder Time A small molecule binding the same orthosteric site engages fewer of those contact points. Not because small-molecule chemistry is weaker, but because a small molecule, by definition, occupies less of the binding region than a peptide does. This model suggests the consequence. The small molecule can show affinity for the site. It can produce binding. What it has more trouble doing is stabilizing the specific active conformation that the full peptide contact network selects for. The orthosteric site is the same site. The conformational outcome accessible from it depends on how much of the binding architecture a ligand can engage at once. Dr. Kenakin frames this carefully in the lecture: an orthosteric small molecule binds in only a few of the regions a peptide engages, and on this model, it will not stabilize the active state the same way. The framing is "seems to be difficult." Not impossible. Not categorically excluded. Difficult, for a reason that is structural rather than chemical. Why Allosteric Modulation Is the Productive Route The same structural account points toward the alternative that has been productive at these targets. An allosteric modulator does not need to engage the orthosteric contact network at all. It binds at a separate site, often on the receptor's extracellular surface or within a transmembrane domain, and influences the receptor's conformational equilibrium from there. The active state can be stabilized through a different geometric route, one that does not require the small molecule to reach across the full peptide binding region. Family B GPCRs have a rich history of allosteric ligands that produce activation. The argument is not that orthosteric small molecules are wrong at these receptors. It is that allosteric chemistry has a structural advantage when the goal is stabilizing an active state at a receptor whose natural agonist is a peptide. What This Means for Program Decisions The affinity-trap account, treated as a model rather than a verdict, has practical implications. It suggests that the difficulty an orthosteric small-molecule agonist program encounters at a family B GPCR may be a feature of the geometry, not a flaw in the chemistry. A series that shows good binding and weak activation, repeatedly, may be encountering the limit of what a small molecule can do at a site optimized over evolutionary time for peptide engagement. It also suggests that allosteric modulation deserves earlier consideration than it sometimes receives at these targets, and that biologic modalities, including peptides themselves, occupy a structural space orthosteric small molecules are not well positioned to fill. These are framing decisions, not prescriptions. The orthosteric site at a family B GPCR is not closed to small molecules. It is, on the affinity-trap account, a more difficult place to produce agonism than the same kind of site at a receptor whose natural ligand is itself small. Why Terry's Corner The affinity-trap account is one framework. The lesson it comes from develops what follows: biased signaling at peptide receptors, antibody-driven control of receptor disposition, the ADME and safety profile GPCR biologic drugs inherit, and the trafficking decisions that determine receptor fate inside the cell. These are pharmacological frameworks, and small-molecule intuition does not transfer cleanly to all of them. Terry's Corner is the room where pharmacologists work through frameworks like these alongside Dr. Terry Kenakin, with structured lessons as the foundation and live AMAs and workshops where the thinking comes alive. This is where receptor pharmacologists who take interpretation seriously sharpen their thinking together. 🟢 40 years of expertise at your fingertips: Explore the complete library ➤ ✳️ Want to know what's inside? Read the latest articles ➤ Stay sharp between lectures. Subscribe to The Kenakin Brief today ➤ Check out the YouTube Channel. https://www.youtube.com/@TerryPharmacologyCorner➤

Dr. GPCR is proud to partner with the 5th Annual GPCRs-Targeted Drug Discovery Summit. This post is your one-stop hub — agenda highlights, who's attending, our exclusive discount code, and speaker interviews as they go live. Why the GPCR Drug Discovery Field Is Converging in Boston The GPCR field is in a genuinely exciting moment. Not hype — momentum. The human genome encodes ~800 GPCRs, yet only around 15% are currently targeted by approved drugs — leaving an enormous and largely untapped therapeutic opportunity. New structural tools, AI-driven design pipelines, and a growing number of programs moving into the clinic are redefining what's possible across modalities and indications. Pharma interest is high, as reflected in major deals across the space. The 5th Annual GPCRs-Targeted Drug Discovery Summit is the industry-led meeting dedicated entirely to GPCR drug discovery — across small molecules, peptides, and antibodies, and across indications. This year's program reflects where science is actually heading. Dr. GPCR founder Dr. Yamina Berchiche will be there — if you're attending, reach out to connect. Who's at the GPCR-Targeted Drug Discovery Summit 2026 The meeting brings together 80+ senior leaders from biotech and pharma to advance GPCR programmes from discovery through translation — experts in GPCR biology, structural biology, computational design, pharmacology, and translational strategy. Companies already confirmed to attend include: Abalone Bio · AbbVie · Biagon · Biolexis Therapeutics · Confo Therapeutics · Eli Lilly · GSK · Nabla Bio · Northeastern University · Nxera Pharma · OMass Therapeutics · Superluminal Medicines · Tectonic Therapeutics · and many more. GPCR Drug Discovery Agenda Highlights: What's New in 2026 This year's summit runs across three days — an AI & ML Focus Day on April 28, followed by two conference days — and the program spans the full breadth of the field. Biased Signaling, Endosomal Pathways & GPCR Signaling Complexity How do we disentangle intrinsic, system, and kinetic bias in a way that actually predicts clinical outcomes? Sessions from InterAx Biotech, Northeastern University, and Function Therapeutics dig into this — moving beyond static potency and efficacy to mechanistic signatures that guide drug design. A panel discussion will tackle best practices for measuring GPCR signaling bias in vitro and what that means for in vivo and clinical translation. AI & ML in GPCR Drug Discovery A dedicated focus day brings together teams from Nabla Bio, Abalone Bio, Biagon, Iambic Therapeutics, Lembas, and Eli Lilly. These aren't primers on AI — they're teams presenting real workflows and real data, covering generative antibody design, dynamic conformational modeling, federated computing platforms, and predictive simulations that shorten discovery timelines. Antibodies, Cyclic Peptides & Allosteric Modulators Nine or more presentations on non-small molecule approaches — including agonistic antibodies, GPCR-directed ADCs, orally available cyclic peptides, and allosteric probes for Class B GPCRs. Companies presenting include Skymab Biotherapeutics, Confo Therapeutics, GSK, Metaphore Biotechnologies, and Abilita Therapeutics. Translational Stories & Clinical Data OMass Therapeutics on long-residence MC2R antagonists. Tectonic Therapeutics on engineering a long-acting relaxin for pulmonary hypertension. Kainova Therapeutics presenting Phase 1 outcomes for their EP4 receptor antagonist in solid tumors. Alphamol on Phase 1 results from an orphan GPCR program pursued against industry skepticism. 🎥 Speaker Spotlight: GPCR Drug Discovery Experts to Watch Dr. Will Barnes is Executive Director and Head of GPCR Biology at Iambic Therapeutics, where he leads AI-driven structural modeling for GPCR drug discovery. With a PhD studying histamine receptors and a postdoc with Bob Lefkowitz at Duke, he brings two decades of industry experience — and a GPCR program in every chapter of it. Watch our conversation below. Chris Dockendorff is the founder of Function Therapeutics, a small biotech on the University of Wisconsin–Milwaukee campus working primarily on protease-activated receptors. A medicinal chemist by training, he has spent his career moving between academia and industry, building small molecules that solve real problems for biologists. At the 5th GPCRs Targeted Drug Discovery Summit, Chris is leading a roundtable on biased signaling, endosomal signaling, and GPCR oligomerization. Watch our conversation below. Register for the GPCR Drug Discovery Summit — Exclusive DrGPCR Discount Use the exclusive DrGPCR discount code DRGPCR10 at checkout for 10% off registration. Early bird pricing also runs through March 6, saving up to $600 off the door price — so don't wait. 🔗 Register here 🔗 Explore the full event guide 🔗 Contact the event team for your discount The 5th Annual GPCRs-Targeted Drug Discovery Summit takes place April 28–30, 2026 at The Colonnade, 120 Huntington Avenue, Boston, MA.

Advance your GPCR research with expert-led Masterclasses on pharmacology, efficacy, signaling, and drug discovery. Built for serious scientists. University / Masterclass On Demand Every Masterclass session. Anytime. At your pace. The full recording library of GPCR Masterclass sessions — revisit the science, catch what you missed, and explore topics at the depth they deserve. On-demand recordings are included inDr. GPCR University Try it for 14 days Recording library Explore the Masterclass library Full recordings of every Masterclass session. Filter by category, level, or instructor to find exactly what you need. Filter by Category Filter by Level Filter by Instructor Watch Now Sudarshan Rajagopal The Spatiotemporal Revolution in GPCR Biology Watch Now Bryan Roth GPCR Molecular Glues: Biased Modulation at the Receptor–Transducer Interface Watch Now Terry Kenakin Unconventional GPCR Ligands Watch Now Sam Hoare How Signaling Kinetics Shapes GPCR Drug Action Watch Now Kenneth A. Jacobson, Matteo Pavan Structure-Based Design of Modulators of Purinergic GPCRs Watch Now Terry Kenakin Designing with Time: GPCR Ligand Kinetics Watch Now Terry Hebert GPCR Signaling in iPSC-Derived Cardiac Disease Models Watch Now Terry Kenakin Assessing Bias: The Practical Approach Watch Now Terry Kenakin From Body to Benefit: Drug Disposition 1 2 3 1 ... 1 2 3 ... 3 Topics covered Deep dives across the full scope of GPCR science Sessions span the entire landscape of GPCR pharmacology, from foundational principles to frontier research. Biased Signaling & Allosteric Modulation Structure-Based Drug Design Innovation & Strategic Application Translational Pharmacology & Disease Models Advanced Quantitative Approaches Translational Pharmacology Innovation & Strategic Application Allosteric Modulation Allosteric Modulation & Kinetics The scientists Learn from world leaders in GPCR research Every session is led by a recognized expert with decades of experience in GPCR pharmacology and drug discovery. Andrew Tobin University of Glasgow Jakob Höppner Endocrine Unit, Massachusetts General Hospital and Harvard Medical School Marsha Pierce Midwestern University Samuel Hoare Pharmechanics LLC Terry Hébert McGill University Yamina Berchiche Dr. GPCR & Yamina's Corner Bryan Roth UNC Chapel Hill Medical School Kenneth Jacobson NIH Matteo Pavan NIH Sudarshan Rajagopal Duke University School of Medicine Terry Kenakin Terry's Corner How it works? Your library. Your pace. 1 Browse or search Filter by scientific category, instructor, or level. Find the session that matches what you're working on right now. 2 Watch at your pace Full recordings with no time limits. Pause, rewind, revisit. The science is here whenever you need it. 3 Go deeper Join the next live Masterclass to ask your questions directly. The recordings are the foundation — the live sessions are where you go further. Want to be in the room live? Live Masterclass sessions run regularly with interactive Q&A. See what's coming up next. See live sessions → What others are saying Dr. Hoare is very experienced in the field. What came as a pleasant surprise was how didactical and well-thought-out his course was—highly recommended. The really unexpected was that the Q&A sessions reached the highest level—beyond excellent. I am a convert! I will keep Dr. GPCR and the offered resources in my work sphere GPCR researcher Thank you for bringing this 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 GPCR researcher The content had enough depth to satisfy the hunger for theory while being full of practical knowledge GPCR researcher The best pharmacology teacher 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 GPCR researcher Dr. Hoare's extensive and elaborative explanation of the topics at hand was excellent and very digestible. Thoroughly enjoyed learning from him GPCR researcher Dr. Kenakin is a leading expert in the field. Aside from his vast experience in drug development, not to mention his extensive publication record, Dr. Kenakin is a masterful teacher and communicator. GPCR researcher About the GPCR Masterclass What is a GPCR Masterclass? The GPCR Masterclass is a live scientific discussion with a leading expert in GPCR pharmacology, receptor biology, or drug discovery. Sessions focus on research questions, experimental interpretation, and emerging challenges in GPCR science. Are the sessions live or recorded? Masterclass sessions are conducted live with an invited expert. After the event, recordings are added to the Masterclass course library, where Premium Members can access them on demand. Who should join? The Masterclass is designed for GPCR researchers, pharmacologists, and drug discovery scientists working in academia, biotech, and pharmaceutical research. Can I watch sessions later if I miss the live event? Yes. All sessions are recorded and available in the Masterclass course library for Premium Members. Can I watch sessions later if I miss the live event? Yes. All sessions are recorded and available in the Masterclass course library for Premium Members. How do I fit this in my schedule? You can attend the live discussion or watch the recording later. The Masterclass library allows members to revisit sessions at any time. What makes the Masterclass different from reading papers or textbooks? The Masterclass focuses on scientific interpretation and discussion. Experts explain how they think about pharmacological data, experimental design, and discovery challenges—insight that is rarely captured in publications. What happens during the live discussion? Each session begins with a focused presentation from the guest expert, followed by moderated discussion and questions from participants. The format allows deeper exploration of pharmacology concepts than typical conference presentations. 200+ sessions are waiting for you inside University The full on-demand library, plus live Masterclasses, premium intelligence, jobs, events, and a community of GPCR scientists — all in one place. See what it feels like... Try University for 14 days — $50

Advance your GPCR research career with Dr. GPCR University. Access 20+ on-demand GPCR courses, 200+ expert talks, weekly news, and a global scientist network. Join Premium today. Dr. GPCR University Your professional home in GPCR science. University is your professional home in GPCR science — premium intelligence, live Masterclasses, job listings, events, and a community of scientists who have your back. Everything you need, in one place. See what it feels like — $49 for 14 days Already know this is home? Join University — $499/year 1,400+ GPCR scientists reached 200+ Expert talks available $499 Per year — less than $10/week What's inside? The rooms in your professional home University isn't a bundle of features — it's a place where your GPCR professional life is supported. Here's what's waiting for you inside. Live Masterclass Live scientific exchanges with leading GPCR experts. You're in the room with the scientist, asking your question — not watching from the audience. Explore Live Masterclass → Job Listings GPCR-specific job opportunities curated for the community. Your next role is already here — opportunities find you when you're inside the ecosystem. Masterclass On Demand Full recordings of every session, available anytime. Revisit the science at your pace — over 200 expert talks in the library and growing. Explore Masterclass on Demand → GPCR Events A calendar of relevant conferences, meetings, and events in the GPCR field. Your next conference is already here. Premium Weekly News The complete GPCR intelligence — classified publications, industry news, job listings, and events calendar. Know what's coming before it becomes consensus. See Weekly News → Ask the Ecosystem The question you've been sitting on — someone in this ecosystem has the answer. A discussion forum where members share insights and get answers from the community. Live Masterclass In the room with the scientist, not watching from the audience Live scientific exchanges where you engage directly with leading GPCR experts. The question you've been holding — this is where you ask it. Dr. Dmitry Veprintsev | U. of Nottingham Biophysical approaches to study orphan GPCR ligand binding and signalling June 18, 2026 Dr. Jakob Höppner | Harvard University | MGH Subcellular Regulation of PTH1R Signaling Translational Pharmacology & Disease Models June 11, 2026 Dr. Andrew Tobin | Glasgow University How to Build Breakthrough GPCR Programs Research Strategy June 4, 2026 Dr. Marsha Pierce | Midewestern University Introduction to GLP-1 pharmacology October 8, 2026 Explore Live Masterclasses → Who it's for? Whether you're just starting out or 20 years in — this is your place University is designed for GPCR scientists at every career stage who want to stay sharp, connected, and supported. 🎓 Early-career researchers Find your footing in the field. Access the experts, the intelligence, and the community that accelerates your growth. 🔬 Discovery scientists Stay at the frontier. Live Masterclasses and Premium Weekly News keep you ahead of the field — not chasing it. 🏆 Senior investigators Your career stage doesn't matter. Your commitment to the science does. Connect, contribute, and stay current. Explore the Masterclass On Demand Watch Now How Signaling Kinetics Shapes GPCR Drug Action Sam Hoare Watch Now The Spatiotemporal Revolution in GPCR Biology Sudarshan Rajagopal Watch Now GPCR Signaling in iPSC-Derived Cardiac Disease Models Terry Hebert Explore Masterclasses On Demand → The comparison A society membership costs more and gives you less Most GPCR scientists belong to at least one scientific society. Here's how that compares to University. Typical Scientific Society $150 – $500+/year A journal subscription A conference discount A newsletter Occasional networking events Dr. GPCR University $499/year — less than $10 a week Live Masterclasses with leading GPCR scientists 200+ on-demand expert sessions Premium Weekly News intelligence GPCR job board and events calendar Community forum & ecosystem access Intelligence Hub dashboard Grandfather guarantee — your rate never increases "The one membership that has your back." $50 for 14 days - Strat Now What others are saying Scientists inside the ecosystem Dr. Hoare is very experienced in the field. What came as a pleasant surprise was how didactical and well-thought-out his course was—highly recommended. The really unexpected was that the Q&A sessions reached the highest level—beyond excellent. I am a convert! I will keep Dr. GPCR and the offered resources in my work sphere GPCR researcher The content had enough depth to satisfy the hunger for theory while being full of practical knowledge GPCR researcher Dr. Hoare's extensive and elaborative explanation of the topics at hand was excellent and very digestible. Thoroughly enjoyed learning from him GPCR researcher The course was very practical and easily translatable to experiments that we could do in our own labs. It was clear that Dr. Hoare is very in touch with the technical and human challenges we encounter in our work GPCR researcher Thank you for bringing this 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 GPCR researcher The best pharmacology teacher 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 GPCR researcher Dr. Kenakin is a leading expert in the field. Aside from his vast experience in drug development, not to mention his extensive publication record, Dr. Kenakin is a masterful teacher and communicator. GPCR researcher Common questions Thinking it over? Fair enough. Here are the concerns we hear most — and honest answers. "It's too expensive." At less than $10 a week, University gives you live access to leading GPCR scientists, 200+ on-demand talks, premium intelligence, a job board, events calendar, and a global community of peers. One insight, one connection, one 'aha' moment — can save months of research time. "I'm not sure I'll use it often." Even one Masterclass or one new collaboration can make a difference. Members often find value in ways they didn't expect — from expert feedback to career-changing introductions. That's why we offer a 14-day trial, so you can experience it first. "I already get what I need from papers." Papers inform. University helps you understand and apply that knowledge — through expert context, structured scientific exchanges, and real interaction with peers from academia and industry. "Will this really help my career?" Yes. Members grow visibility, confidence, and connections that open doors. It’s not just about learning — it’s about being seen, supported, and part of something bigger . Frequently asked questions What is Dr. GPCR University? Dr. GPCR University is an educational platform that provides in-depth learning and training resources on G protein-coupled receptors (GPCRs). At Dr.GPCR University, you’ll find: Courses: Dive deep into curated educational content designed by experts in GPCR research. Our courses provide comprehensive, on-demand learning to help you expand your knowledge and stay current in the field. Symposia Engage with leading scientists through our symposia, featuring in-depth discussions on cutting-edge research and breakthroughs in GPCR science. Each session brings together a community of experts to share insights and advancements. Summit A global gathering of researchers and professionals showcasing the latest developments in GPCR research. Participate in presentations, networking opportunities, and collaborative sessions. Virtual Café Listen to casual, interactive discussions with experts in the field. How do I register for Dr. GPCR University Masterclasses? To register for any course, you must have a FREE Ecosystem member account. We carefully screen anyone signing up to ensure they are real humans working on GPCRs, so you might not receive confirmation immediately. When signing up for the first time, try to complete as much information as possible about yourself. Who are the Dr. GPCR University Masterclasses designed for? The classes are designed for researchers, students, and professionals in biology, pharmacology, and biochemistry, but anyone interested in GPCR research is welcome to join. What topics are covered in the masterclasses? Masterclasses cover a variety of track including but not limited to pharmacology foundations, agonists, antagonists & core mechanisms , allosteric modulation & kinetics, advanced quantitative approaches and innovation & strategic application Can I register my team for a Dr. GPCR University Masterclasses? To register as a team, one of you must be a Premium Member. This person must email hello@drgpcr.org indicating how many people will register for the course, the names of the participants, and their emails. We will contact each person individually to help them set up a FREE Ecosystem Membership. They will be asked to join a private group to keep updated with the latest announcements about the course. Are the masterclasses on-demand or live? 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Explore detailed information about our GPCR-focused University Courses. Learn about course content, instructors, and how to advance your expertise in drug discovery. Empower. Connect. Transform. Become part of the Dr. GPCR University Instructor community—where teaching is more than sharing knowledge; it’s about uplifting scientists and advancing GPCR discovery, together. Connecting scientists through knowledge, passion, and purpose. About Dr. GPCR University Dr. GPCR University is a global platform where scientists share their knowledge, inspire discovery, and advance GPCR research together. Our on-demand courses connect experts, students, and industry professionals through authentic, instructor-led learning—built by scientists, for scientists. Each contribution brings new perspectives and tools to advance the field. Instructors are recognized and compensated for their work, ensuring that every shared insight creates impact, visibility, and lasting value across the GPCR community. Course Formats You Can Teach At Dr. GPCR University , every instructor brings a unique voice, style, and rhythm to teaching. Our flexible course formats are designed to fit your time, depth, and teaching goals — whether you’re sharing a focused insight or leading a full exploration of GPCR science. You can also co-lead Full-Length Courses with up to three fellow instructors to share the workload and enrich the learning experience. 🧭 Full-Length Course Structure: 4 × 1-hour sessions Purpose: Deep, multi-session learning experience Best for: Comprehensive topics that require exploration and discussion ⚡ Short Course Structure: 1 session (2–4 hours of content) Purpose: Concise yet thorough coverage of key concepts Best for: Core methods, applied principles, or emerging topics 🔍 Mini Course Structure: 1 short lesson (1–2 hours of content) Purpose: Focused insights into a single theme Best for: Quick takeaways or specialized topics No matter the format, your course helps scientists learn, connect, and keep GPCR science moving forward — one discovery at a time. Instructor Benefits At Dr. GPCR University , we believe those who teach move science forward. As an instructor, you’re not just sharing knowledge — you’re shaping the next generation of GPCR scientists. We make sure your time, expertise, and contribution are recognized and supported every step of the way. 🌟 By teaching with us, you gain: ✔ Premium Membership for you and your team for one year (no credit card required) ✔ A global platform to share your expertise and reach scientists worldwide ✔ Full support with technical setup, editing, and course promotion — so you can focus on teaching We handle logistics so you can focus on what truly matters: delivering meaningful, high-quality education. To ensure lasting impact, each course becomes part of the Dr. GPCR University ecosystem — maintained, updated, and accessible to learners in the long term. Your name and expertise remain at the heart of the course, continuing to inspire scientists long after the sessions end. Together, we’re shaping the future of GPCR education — one course, one scientist, one discovery at a time. What You’ll Need to Provide to Teach a Course Welcome — we’re thrilled to have you join Dr. GPCR University . You bring the expertise; we’ll handle the setup, editing, and promotion. Here’s everything you’ll prepare to bring your course to life: 🧩 Step 1: Email us Start by emailing it us at Hello@DrGPCR.org . We will then have a short call and send you the our Instructor Intake Form — it’s how we build your profile and course page. You’ll be asked for: Instructor info – name, email, affiliation, short bio, photo, and optional social media handles. Course details – title, format (short talk / mini-course / series), audience, main objectives, expected learning outcomes, key topics (≈ 250 words), recommended readings, and any co-instructors. Preferences & agreement – communication style, access to the Premium area, and acknowledgment of the instructor agreement (you’ll receive the full version right after submission). 🧱 Step 2: Plan Your Course Structure Decide how your course will flow — number of modules, duration, and teaching style. (See Course Formats above for ideas.) 🕙 Scheduling note: Courses are typically hosted Thursdays at 10 AM EST — a sweet spot for our global community. We’ll confirm your date together once your proposal is approved. 📝 Step 3: Prepare Your Content Create your teaching materials — slides, visuals, readings, or anything that helps learners grasp your message. Don’t worry — we’ll support you with templates and review tips along the way. 🎥 Step 4: Record a Short Video Chat You’ll have a quick recorded conversation with Dr. Yamina Berchiche about your course — what it covers, why it matters, and what students can expect. It’s relaxed, engaging, and helps introduce you to the community. 💬 Step 5: Join Your Private Course Group Once live, you’ll connect with your students in a private discussion space — perfect for questions, insights, and follow-ups. 💫 Step 6: Teach & Inspire Share your expertise with scientists around the world. Enjoy the experience, the visibility, and the impact — and receive recognition and compensation for your contribution. (See Instructor Benefits for details.) ✨ Your ideas, your voice, and your course will help shape the next chapter of GPCR discovery. Share Your Expertise with the World We’re here to support you from idea to impact. Start your journey as a Dr. GPCR University Instructor and help move GPCR science forward. Email us at Hello@DrGPCR.org Live Masterclass Sessions Previous Instructors Andrew Tobin Marsha Pierce Terry Hébert Bryan Roth Matteo Pavan Terry Kenakin Jakob Höppner Samuel Hoare Yamina Berchiche Kenneth Jacobson Sudarshan Rajagopal Dr. GPCR Courses Reviews Dr. Hoare is very experienced in the field. What came as a pleasant surprise was how didactical and well-thought-out his course was—highly recommended. The really unexpected was that the Q&A sessions reached the highest level—beyond excellent. I am a convert! I will keep Dr. GPCR and the offered resources in my work sphere GPCR researcher Thank you for bringing this 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 GPCR researcher The content had enough depth to satisfy the hunger for theory while being full of practical knowledge GPCR researcher The best pharmacology teacher 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 GPCR researcher Dr. Hoare's extensive and elaborative explanation of the topics at hand was excellent and very digestible. Thoroughly enjoyed learning from him GPCR researcher Dr. Kenakin is a leading expert in the field. Aside from his vast experience in drug development, not to mention his extensive publication record, Dr. Kenakin is a masterful teacher and communicator. GPCR researcher The course was very practical and easily translatable to experiments that we could do in our own labs. It was clear that Dr. Hoare is very in touch with the technical and human challenges we encounter in our work GPCR researcher Contact Contact us First name* Last name Email* Write a message Submit