The next edge in discovery isn’t louder exposure—it’s smarter engagement. This week’s Dr. Kenakin from Terry's Corner shows how to tame irreversible drugs so their kinetic power works for you, not against you. You’ll get a framework to predict duration, penetration, and PK/PD separation—so decisions move faster and risks surface earlier. Breakthroughs this week: nanomedicines targeting PAR2 for sustained analgesia; Emerging Voices in GPCR Biology;

This session unpacks how persistent binding can either accelerate your program—or quietly kill it. That’s the power (and the peril) of irreversible drugs. These aren’t just “stronger binders.” They’re kinetic game-changers—compounds that rewrite the relationship between ligand, receptor, and physiologic outcome. Understanding how persistent binding affects receptor turnover, tissue penetration, and PK/PD relationships can give your team a strategic edge.

Discover how Dr. Eric Trinquet, creator of HTRF and IP-One assays, turned failure into breakthrough tools for GPCR science. Learn why play, serendipity, and partnerships fuel innovation—and how this mindset can transform your research and biotech career.

Every drug you design will meet an enzyme before it meets its receptor. If you want your molecules to survive first contact with biology—and with the FDA—enzyme inhibition must be part of your core playbook. This week’s feature breaks down exactly how to think about inhibitors with rigor and speed, so you can make better decisions earlier in the pipeline. Breakthroughs this week: Potentiation of GPCR signaling by ATP and sugar monophosphates; Pharmacology 2025; Nxera Pharma

Before your GPCR ligand ever meets its receptor, it meets the enzymes that determine whether it survives long enough to act. Recognizing, predicting, and leveraging these interactions is the essence of enzyme inhibition pharmacology—the framework that connects molecular survival to clinical success.

If you want cleaner decisions, start with the system—then the ligand. This week’s lead feature unlocks a deceptively simple lever that separates signal from storytelling, moving programs forward with fewer surprises. That’s precisely what Terry’s Corner delivers: practical tools from Dr. Terry Kenakin to elevate your science and sharpe It’s a curated toolkit designed to help GPCR professionals move faster, with more confidence. Premium Members count on this every week—and t

What it really takes to launch a GPCR product—years of failure, science, and strategy. Go behind the scenes of pH-Sense with Revity’s Dr. Eric Trinquet.

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...