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

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

This week's Terry's Corner with Dr. Terry Kenakin delivers a game-changing framework for teams grappling with the gap between in vitro potency and in vivo performance.

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

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

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

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.

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...

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

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

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

Hello Dr.GPCR readers! This is Lucía from the Celtarys Research chemistry team.  For our very first post in this ecosystem, we wanted to...

September 2022 "The diamondback moth (Plutella xylostella) is one of the most destructive lepidopteran pests of cruciferous vegetables,...

GPCRs Are Optimal Regulators of Complex Biological Systems and Orchestrate the Interface between Health and Disease GPCRs arguably...