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

Dr. Alex Serafini turned chronic pain into a research mission. Discover how personal experience shaped his work on GPCRs, RGS proteins, and new pain models.

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

Kenakin’s kinetic insights help you translate assay readouts into actionable knowledge that keeps your programs focused and moving efficiently toward clinical relevance.

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.

Sokhom Pin explains why staying in GPCR research during its “unpopular” phase helped him become a sought-after expert today.

Sokhom Pin shares how he built a thriving GPCR research team at Alkermes through trust, culture, and empowerment-driven leadership.

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

Our CSO, Maria, has recently traveled to the US to attend the ACSMEDI-EFMC Medicinal Chemistry Frontiers 2025 , a conference organized by...

Sokhom Pin shares how he earned a PhD while working in biotech, designing a custom program that defied academic convention.

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...

In Terry Kenakin’s latest foundational lesson from Terry’s Corner, he unpacks the art and science of pharmacologic modeling. This isn’t just theory—it's the essential framework used to interpret experimental data, anticipate system-wide drug effects, and design smarter trials.

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

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

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

If you’ve read our previous post, you probably know what CELT-335 is and its high affinity for the cannabinoid 1 receptor (CB1R). During...

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...