Insights That Move the GPCR Field Forward

Every delay in the discovery pipeline compounds into wasted years, lost opportunities, and soaring costs. For drug hunters working at the GPCR interface, the difference between a successful lead and a dead-end candidate often comes down to one overlooked factor: system sensitivity and how we control it.

Each edition highlights the decisions that move GPCR projects forward—from pharmacology essentials to ligand binding site strategies, bench-ready tools, and industry momentum shaping GPCR pipelines. Read fast, apply faster, and stay ahead in GPCR drug discovery with evidence-based insights—no hype, just strategies you can use.

The difference between orthosteric vs. allosteric mechanisms isn’t just academic — an orthosteric antagonist can hijack receptor physiology, while an allosteric modulator works with the system. That choice determines whether you risk over- or under-dosing, miss safety windows, or miss therapeutic breakthroughs.

A powerful new tool tracks GPCR internalization in native cells—no imaging, no overexpression. Learn how pH Sense changes the game for drug discovery.

This week’s insights give you a strategic edge across the pipeline—from drug design that accounts for physiological counterforces, to simplifying internalization detection without microscopy, to boosting HTRF assay sensitivity using fluorescent ligands. It’s a curated toolkit designed to help GPCR professionals move faster, with more confidence. Premium Members count on this every week—and this is your preview.

Choosing the right fluorescent tools is important for the success of drug discovery, just as much as choosing the right targets. One of the best tools to study therapeutic targets are fluorescent ligands, which are very useful in GPCR drug discovery, starting from hit and lead validation all the way to pre-clinical assays. Some of the advantages of using fluorescent ligands for this are

GPCRs don’t play fair. Learn how opposing processes, receptor trafficking, and constitutive activity shape drug response—and how to design for them.

Boston, MA – September 2025 — Dr. GPCR, the global nonprofit platform dedicated to advancing GPCR science through education, community, and platform visibility, is proud to spotlight pHSense™, a new reagent family from Revvity, now featured across the Dr. GPCR Ecosystem.

Early signals can mislead. This week’s Dr. GPCR Weekly shows how to call Mechanism of Action with model-first rigor—distinguishing orthosteric vs. allosteric, designing assays that reveal mechanism, and unlocking SAR. Plus: Novo’s \$550M obesity/diabetes push, Rhythm’s sNDA, key events, and confocal imaging that respects function. Upgrade to Premium for the full digest.

What is Homogeneous Time-Resolved Fluorescence (HTRF)? HTRF is a hybrid detection technology that combines Förster Resonance Energy...

Learn how ligand binding kinetics reveal hidden drug effects, improve GPCR assay design, and prevent costly errors in drug discovery pipelines.

Early signals can mislead. This week’s Dr. GPCR Weekly shows how to call Mechanism of Action with model-first rigor—distinguishing orthosteric vs. allosteric, designing assays that reveal mechanism, and unlocking SAR. Plus: Novo’s \$550M obesity/diabetes push, Rhythm’s sNDA, key events, and confocal imaging that respects function. Upgrade to Premium for the full digest.

Flow cytometry, a laser-based method, is used to examine single cells suspended in a fluid. By measuring the way these cells scatter...

Turn assay snapshots into predictions. Models separate orthosteric vs allosteric mechanisms and guide experiments for faster decisions in Terry’s Corner.

Ajay Yekkirala’s journey from rejected med student to GPCR biotech founder shows how failure, mentorship, and curiosity can drive real innovation in drug discovery.

Curve shifts can mislead, but statistics won’t. This week in Terry’s Corner: power analysis, t-tests, ANOVA, and F-tests to move from “I think” to “I know.” Plus, Ajay Yekkirala on AI-driven GPCR therapeutics and an invitation to Boston’s GPCR Happy Hour. Premium Members get full access to curated jobs, events, and must-read publications—your edge to stay ahead in fast-moving GPCR science.

Applications of Fluorescent Probes in Confocal Imaging of GPCRs: From Live to Fixed Cells GPCRs are present across cell membranes...

Stop guessing at curve shifts. Learn how t-tests, ANOVA & F-tests bring confidence, not noise, to drug discovery decisions.

Purpose-driven science works because it creates resilience. Careers built on prestige, titles, or external pressure can burn out quickly. But careers built on urgency, alignment, and meaning are the ones that last.

This week’s Dr. GPCR Weekly News delivers urgent insights every GPCR scientist and drug discovery leader needs. From Terry’s Corner on the hidden traps of allosteric binding, to Yamina’s Corner on the hidden costs of fragmented systems, and a preview of Discovery on Target 2025, this edition highlights the frameworks shaping the next decade of therapies. Plus: industry breakthroughs on metabolic GPCRs, key September events, curated career opportunities, and must-read publicat

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!

The ability to identify compounds that interact with molecular targets involved in disease pathways is where the development of new...

At its core, Catherine Demery’s research is about receptors and signaling pathways—how mu-opioid and alpha-2 adrenergic receptors interact to disrupt breathing. But it’s also about public health urgency.

Think you understand ligand displacement? Think again. This week’s Terry’s Corner blog reveals how allosteric modulators reshape receptor identity—and why conventional binding logic fails in these systems.