In this 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.

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.

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.

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...

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.

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.

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.

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

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.

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

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.

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.

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.

Assay development is more than synthesis. Discover how Celtarys is helping scientists solve GPCR research challenges.

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

Dr. Maria Majellaro shares the pivotal moments that shaped her career, from chemistry tests to launching a biotech company changing GPCR research.

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

How Maria Majellaro transitioned from medicinal chemist to biotech CSO, and how Celtarys is now advancing GPCR research tools with Dr. GPCR.

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

Today’s GPCR researchers want multiplexing, miniaturization, and scale. Here’s the toolkit delivering just that and why it matters now.

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

Dr. Sakmar reveals how activating GPCR autoantibodies could be driving disease—and how new tools make them detectable.

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

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