space focused on GPCR pharmacology. Explore her path from postdoc to platform builder.   PK/PD   Subscribe to The Kenakin Brief Fluorescent Probe CELT-419 Powers D3R Binding Assays Across Platforms GPCR Podcast appearance. GPCR Team

s latest lecture delivers high-impact insight crafted for teams navigating the complex behaviors of GPCR-targeting As Kenakin explains, all GPCR signaling is allosteric , and pretending otherwise introduces risk at every You’ll see how this manifests in real data from muscarinic receptors, CCR5 chemokine programs, and NMDA Interpret probe-dependent effects Model and anticipate longer equilibration times Recognize when your data Corner  is your trusted, expert-led guide through the evolving landscape of GPCR science.

Hello GPCR Enthusiasts, Interpreting binding data isn’t optional—it’s career-defining. Yamina’s Corner reveals how fragmented data, undefined workflows, and ambiguous decision gates silently Stop wasting talent:  When senior leaders spend nights copy-pasting data, your burn rate accelerates Read the article now ➤ Discovery on Target - The Next Wave of GPCR Drug Discovery The 20th Annual GPCR-Based GPCR Premium Membership Gives You an Edge The GPCR field is advancing at breakneck speed.

GPCR is proud to partner with the 5th Annual GPCRs-Targeted Drug Discovery Summit. Why the GPCR Drug Discovery Field Is Converging in Boston The GPCR field is in a genuinely exciting moment These aren't primers on AI — they're teams presenting real workflows and real data, covering generative antibody design, dynamic conformational modeling, federated computing platforms, and predictive simulations Translational Stories & Clinical Data OMass Therapeutics on long-residence MC2R antagonists.

Industry insights: Confo nominates SSTR5 agonist antibody CFTX-2034; Lilly oral GLP-1 maintenance data Full course videos stream directly from the platform, and downloadable resources are available in one Why this matters now: Stop wasting time hunting for relevant training across fragmented platforms. Interpret cytotoxicity data correctly—distinguish transient stress from meaningful off-target damage. More data. More companies. More noise.

Must-read publications:  GPCRs in neurological disorders; OSTα-OSTβ structure; GPCR–G protein–β-arrestin GPCR Ecosystem The Ecosystem has been evolving over the years—expanding into an integrated platform for GPCR podcast , Dr. GPCR innovation is accelerating. GPCR Team

It involved making sense of messy data and realizing the power of not knowing . For innovators building tools, platforms, or therapeutics, these origin moments are where tomorrow’s Luck, Leadership & GPCR Signaling Michelle is clear: luck played a role. But so did choice. GPCR Podcast 🔓 Want to go deeper? Join   Dr. GPCR Premium  for exclusive tools, deep dives, and expert access.

The GPCR Happy Hour Room What struck me first was the range. GPCR Happy Hour is free to every scientist who walks in. GPCR YouTube channel, and I encourage you to watch it. GPCR: welcome. This is what we do. Come find us in the fall. the people https://www.ecosystem.drgpcr.com/gpcr-university

The Cell Surface Is Only Part of the Story For decades, GPCR pharmacology centered on events at the cell Work on receptors such as GLP-1R and MC4R has demonstrated that internalized GPCRs can continue to signal This finding reframes how internalization data should be interpreted. Terry Kenakin’s session on measuring GPCR internalization walks through the assay logic, the mechanistic distinctions, and the interpretive frameworks that connect trafficking data to therapeutic decisions

Why GPCR Drug Discovery Is More Complex Than It Looks G protein-coupled receptors (GPCRs) have long occupied Allosteric Modulation and the Microcircuit Model of GPCR Pharmacology Understanding GPCRs as allosteric Emerging Families and Orphan GPCRs: Expanding the Drug Discovery Target Space Family A and B GPCRs — Eurofins DiscoverX has developed an extensive platform of GPCR functional assays — including β -arrestin It also requires alignment between in vitro   GPCR assay  data and pharmacokinetic measurements.

The central role of GPCRs in Neurological Disorders GPCRs are the largest family of membrane receptors Over 30% of FDA-approved drugs target GPCRs, with many targeting CNS located GPCRs. GPCR Structure, Activation, and Signaling Pathways in the Brain An understanding of GPCR structure is GPCR signaling: (A) an orthosteric ligand (orange) binds an inactive GPCR, the β2 adrenergic receptor Emerging GPCR Therapeutic Targets in CNS Drug Discovery GPCRs have been studied for decades, but there

Get your space suits on, GPCR cadets! up with a series of cosmic GPCR events for the year ahead. It’s time to mark your calendars and save the dates—let’s make some stellar memories together! Discounted GPCR courses - because who doesn't love a good deal?  Classified GPCR News  Let’s dive into the   Classified GPCR News from October 28th to November 3rd, 2024

Welcome GPCR Fans,   Every discovery-phase decision you make shapes your entire pipeline trajectory—and Must-read publications:  GPCRchimeraDB: Database of engineered GPCR designs. Stay ahead of competitors:  Know when your data reflects equilibrium and when to probe deeper, ensuring GPCR University Course Attendee Dr. The pace of GPCR innovation is accelerating.

Breakthroughs this week: C. elegans avoids EGCG via SRXA-7 GPCR; a bidirectional GPCR switch modulates Design for translation:  Map sensitivity ranges to tissue contexts so your plate data predicts what happens Eric Trinquet traces how a series of bold pivots—from Cisbio’s HTRF platform to IP-One and now pHSense—reshaped how GPCR biology gets measured. GPCR innovation is accelerating.

With limited structural data but a growing pharmacological interest, GPCRs presented the perfect challenge This success was a revelation—it was possible not only to interpret experimental data but to forecast Trainees must learn how to interpret assay data, understand pharmacological context, and communicate Still, he emphasizes that data limitations remain a major challenge, especially when it comes to small Unlike protein sequences, small molecule data are often fragmented, inconsistent, or unavailable, making

If you’re building tools or careers in GPCR science, this is your playbook. It took data, yes—but also a deep partnership with GPCR legend Terry Kenakin to bridge industry credibility constitutive activity, agonist-induced internalization, and cellular dynamics. 🔄 What Changed After This Data GPCR   Dr. GPCR X Revvity Collaboration ⸻ Want more like this? 👉 Join the Dr. GPCR Premium Ecosystem  for behind-the-scenes access to GPCR innovators, exclusive deep-dives, and practical

Welcome back GPCR Fans, Clean data can still mislead if the underlying assumptions aren’t tested. Watch the trailer 👇 What you’ll gain Validate the model behind the data.   an Innovation Engine From Pipettes to Platforms: The Evolution of GPCR Research How GPCR Spatial Signaling With live GPCR University courses returning next year and platform capabilities expanding, Premium pricing before the change is fully grandfathered  — your rate stays locked, and your whole team benefits as the platform

Before your GPCR ligand ever meets its receptor, it meets the enzymes that determine whether it survives Discovery Program So what does that mean for discovery scientists designing the next generation of GPCR Even the most elegant GPCR ligand can fail if it never reaches its receptor. This lecture challenges scientists to move beyond binary inhibition data and embrace a systems-level Kenakin with your own enzyme or GPCR interaction puzzles.

Introduction G protein-coupled receptors (GPCRs) don't simply switch on or off. selectivity of retratutide for GLP-1 receptor over GIP receptor compared to tirzepatide and yields sufficient data This data is calculated from the estimated max and EC50. For further reading on GPCR biased signaling and assay methodologies, explore the ‘Insights into GPCR Visit Eurofins DiscoverX GPCR Products and Solutions to explore the full portfolio of GPCR assays from

Generic cell systems (usually) generate clean data — but they don't reflect the tissue environment, disease The data they generate reflects the cellular background of the expression system, not the tissue or disease The data that's too early to present but too important not to discuss. GPCR University Learner About Dr. GPCR Dr. GPCR is the intelligence and community platform for GPCR scientists.

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 GPCR. GPCR  is a global nonprofit platform advancing GPCR research  through education, community, and platform assay platforms. 🔍 Learn More → Listen to the Podcast with Revvity’s Eric Trinquet → Explore the pHSense

In some models, additional G-protein chimeras further enhance coupling efficiency, creating a robust platform Calcium dose response curves and FLIPR trace data from ChemiSCREEN cell Top. FLIPR trace data from a representative ChemiSCREEN cell line calcium assay with agonist addition at 10 Why GPCR Calcium Assays Remain Valuable A GPCR calcium assay offers several advantages that have made Note the antagonist data retains the vast majority of the assay window seen in the agonist curve.

isn't just  about the latest and best assay; it's about the framework that ensures the right assay data GPCR, we recognized this core problem. We'll look at how overlooked operational details, such as misaligned data from diverse GPCR assay types Part 2: The Data Disconnect : Discover how fragmented, unmanaged GPCR data  cripples scientific progress Learn how to build an integrated data pipeline  that transforms this chaos into a strategic asset.

GPCR. Dear Dr. We’re redesigning the platform for smoother navigation  and preparing to relaunch Dr. GPCR isn’t just a digital platform — it’s a community. GPCR About Dr. GPCR Dr. GPCR is a global platform dedicated to connecting GPCR scientists, industry experts, and innovators through

GPCR community live this week to examine what happens when GPCR selectivity is encoded not at the receptor GPCR University iPSC-Derived Systems for GPCR Signaling and Translation HEK293 systems are powerful tools GPCR University Terry's Corner AMA — How Important Is It to Know Where Your Molecule Binds? interactions — and with it, how we think about drug discovery at GPCRs. GPCR Dr. GPCR is the intelligence and community platform for GPCR scientists.

How a Collaboration Led to a GPCR Imaging Breakthrough JB didn’t set out to contribute to a GPCR imaging When David later shared early data — including a moment where he realized he could image an entire islet It was the start of a scientific partnership with the potential to shift how GPCRs could be visualized Designing Reliable GPCR Imaging Tools for Real Biological Systems Success brought new challenges. What started as one molecule request is now a platform vision — a future where any GPCR could be illuminated

This was more than data. It was ignition. discovery — the instant where the experiment stops being data and starts being meaning. Feeling the urge to take phone pictures of super-resolution data and send them to collaborators because They exchanged instincts as much as data, and built a shared rhythm of problem-solving.  🎧 Listen to the full episode https://www.ecosystem.drgpcr.com/dr-gpcr-podcast/chemical-probes-for-gpcr-imaging-and-internalization

Why Speed Matters in GPCR Drug Discovery Nine out of ten GPCR programs stall  not because the target GPCR Kinetics: The Critical Data You Can’t Afford to Skip Equilibrium potency data only tells part of “GPCRs are nature’s prototype allosteric proteins. Everything they do is allosteric.” Kenakin with your own enzyme or GPCR interaction puzzles. This AMA helps you read that story faster, so you don’t just generate data—you generate direction. 🟢

Broichhagen aka JB, the goal was bold and elegant: Create a photo-switchable ligand to remotely control GPCR They had a tool that did bind the GPCR… but not in the light-controlled way they wanted. Most labs would have stopped there — archived the data, moved on, written it off as a failed bet. “Negative data” isn’t negative — it’s directional. What Changed After This Data This imaging tool is now being used to: Re-evaluate where GLP-1 and GIP

Hi GPCR Community, If you work on GPCR discovery, you already know: early signals can mislead, and timing This week, we focus on how to convert ambiguous data into confident, defensible Mechanism of Action calls—before Career opportunities:  Research Assistant; Postdoctoral Associate; Senior Scientist, Data Science—curated GPCR scientists, translational pharmacologists, biotech discovery teams, platform company leaders, and community platform to help train and inspire the next generation of scientists.