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Thus we propose the use of fluorescent probes in GPCR screening assays due to their numerous advantages The advantages of Fluorescent Probes in GPCR assays over other methods Fluorescent ligands are made by The traditional binding assays for GPCRs use radioligands, whose limitations, especially safety concerns At Celtarys, we focus on developing fluorescent tools that keep minimal background signal even without common starting point for employing fluorescent probes in GPCR assays.

Enhance your GPCR research with deeper assay insights for more effective results. Breakthroughs this week: C. elegans avoids EGCG via SRXA-7 GPCR; a bidirectional GPCR switch modulates Terry's Corner – Assay Volume Control in GPCR Drug Discovery This week in Terry’s Corner, you’ll learn But behind every “new” assay is a decade of design, failure, and rethinking. GPCR innovation is accelerating.

For GPCR assay developers, HCS supports:  Quantitative visualization of receptor internalization and have historically been the standard for GPCR pharmacology. phenotypic screens and targeted GPCR binding studies. the gold standard for image-based GPCR assays. development expertise.

GPCR and Revvity. Every GPCR assay that makes it to market carries years of failures, late-night ideas, risky bets, and Functional assays for GPCRs—especially Gq-coupled receptors—were notoriously messy. Calcium flux? took a risky bet: develop a functional readout for Gq signaling without relying on calcium. internalization assays without imaging.

Radioligands have been used to study GPCRs for decades, but with the advances in the fluorescence field that offer an alternative to radioligands in binding assays. design for specific targets:  Not all targets have available high-affinity radioligands, but with the development GPCR-radioligand binding assays. Fluorescent ligands: Bringing light to emerging GPCR paradigms.

For drug hunters working at the GPCR interface, the difference between a successful lead and a dead-end For GPCR drug discovery, those hidden details can determine whether a compound advances or stalls. The Hidden Lever in GPCR Research In GPCR pharmacology, the conversation often centers on ligand properties—affinity It’s about revealing therapeutic liabilities before  they derail development. between a high-affinity/low-efficacy agonist  versus a high-efficacy agonist  before entering costly development

Eric Trinquet, a veteran innovator behind functional GPCR assays like HTRF and IP-One, believes rigid Why This Matters: IP-One helped set a new gold standard for functional GPCR assays—shifting how compounds Originally developed as ultra-bright lanthanide probes, the team realized they could tune these molecules Mini Timeline 🎯 Early 2000s: Trinquet leads IP1 & Tag-lite development 🧪 Mid-2010s: Rare-earth scaffold Product development isn’t just about science.

Enhancing HTRF Assay Performance in GPCR Research Using Fluorescent Ligands GPCRs are involved in numerous physiological processes, making them a key target in drug development.   This has been done in assays tracking IP1 and cAMP to detect biased agonism in GPCR ligands Table 1. In a recent study , we contributed to the development of a robust HTRF assay for the discovery of new By combining deep expertise in GPCR biology with advanced fluorescence chemistry, Celtarys custom-developed

GPCR – Precision Tools for GPCR Assays Dr. GPCR and Celtarys Research have teamed up. features a discussion about a scalable GPCR-RAMP assay. Their global resource is now helping labs decode GPCR biology at scale. It’s exciting to see how the GPCR field is evolving. GPCR Team

The assays are running, data is flowing in from your CROs or your internal labs , yet progress stalls This disconnect frequently leads to: Underperforming assays. I'll help write CRO scopes, meticulously review assay data, flag risks early, and keep your programs Systems That Drive Progress:  From assay tracking to data workflows, I design simple, scalable tools GPCR As the co-founder of Dr.

to identify compounds that interact with molecular targets involved in disease pathways is where the development Target-based screening is now a fundamental pillar of drug development, and GPCRs are key targets for How Fluorescence Polarization Assays Work: Principles and Applications in GPCR Research FP assays work Compatible with various sources of GPCRs. polarization technology is expected to expand its role in GPCR research through the development of novel

 are interpreted—and how those interpretations quietly shape SAR, lead selection, and development timelines By walking through saturation curves, displacement assays, stoichiometry pitfalls, and kinetic traps, than undermine—lead selection and development timelines. Research , leaders from academia and biotech unpack what effective collaboration really looks like when developing event alerts, and career-relevant opportunities—organized to support real decisions in discovery and development

Docking scores were meaningless without assays. Chemistry fuels assays. Assay data flows back into models. The GPCR Challenge What makes collaboration non-negotiable in GPCR research is the biology itself. , and assay data cycling back to refine predictions. GPCR Models Don’t Discover Drugs—People Do In GPCR research, the biggest breakthroughs won’t come from

August 2022 In vitro assays for the functional characterization of (psychedelic) substances at the serotonin More specifically, this review covers assays to monitor the canonical G protein signaling pathway (e.g recruitment or signaling, and assays to monitor receptor conformational changes. mechanism and linked to its specific execution, as these may heavily impact the assay outcome." Read more at the source #DrGPCR #GPCR #IndustryNews 5-HT2AR, GPCR, hallucinogens, in vitro assay, psychedelics

Is Your GPCR Program Slowing Down—Even With Good Data? You’re not alone. I call it the Lego Bucket Problem : You’ve got CRO output, internal assay data, maybe even some promising arrives too fast and too fragmented CROs deliver output without clear integration Teams chase the wrong assays Here’s what I bring: Biology-First Strategy I’ve designed GPCR assays, led collaborations across research GPCR, I’m connected to 1,300+ scientists and decision-makers worldwide.

Watch Episode 176 The first time Michelle ran a cyclic AMP assay, she did it with a single-channel pipette Assay samples were layered on trays of ice. These weren’t quaint inconveniences. We were doing assays on ice, pipetting one sample at a time. Those early cyclic AMP assays weren’t just cold and slow — they were part of a bigger puzzle. GPCR Podcast 🔓 Get tools, deep dives, and exclusive insights with   Dr. GPCR Premium .

Be Part of the GPCR Community Dr. GPCR is a nonprofit global community  dedicated to building a strong, connected GPCR ecosystem. Leveraging decades of experience, their services include AI-driven target identification, target validation, assay development, compound management, and high-throughput screening in both 384- and 1536-well formats. platform, iPSC-derived models, optogenetics, and high-content screening techniques such as cell painting assays

Celtarys Research expands its assay tools with CELT-419 for D3 receptor studies, and Dr. fuel confidence and fluency Move beyond theory to apply selectivity, ADME, and early safety in real development translational PK/PD   Subscribe to The Kenakin Brief Fluorescent Probe CELT-419 Powers D3R Binding Assays With strong signal stability, HTS compatibility, and broad assay versatility, CELT-419 is designed for GPCR Team

than the assay implied. His work shows why chemical design can outperform antibodies and how rigorous assay validation bridges Programs: Overcoming Assay Limitations with Fluorescent Ligands High-content screening (HCS) is now But HCS only works when assays are built with rigor and powered by the right fluorescent ligands. a robust, reproducible HCS pipeline How fluorescent ligands strengthen specificity, relevance, and assay

mutated GPCRs. , and concise reads on β-agonists, phospho-barcodes, and GPCR allostery. Whether you’re building assays or a scientific career, this is a must-read on why risk, surprise, and Biosensors make once-invisible dynamics assayable at scale. Read the roundup ➤ Why Dr. The pace of GPCR innovation is accelerating.

When assays behave unpredictably, the wrong interpretation doesn’t just waste time; it costs viable compounds , credibility, and millions in development risk. Career opportunities:  Postdocs in GPCR biophysics and assay development; industry scientist roles at Protect your pipeline:  Misinterpreting displacement curves in allosteric assays means discarding viable Aside from his vast experience in drug development, not to mention his extensive publication record,

Imagine running a calcium assay and discovering your compound shows only weak activity. 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. with strategic clarity. 📍 Foundational Level | Calcium Assays 📚 Part of Terry Kenakin’s Pharmacology Unlock "Calcium Assays" now

blood-brain-barrier (BBB) and the complexity of the central nervous system (CNS) pose a challenge for developing Both orphan and well-characterized GPCRs are untapped opportunities for drug development targeting CNS Faster assay development: also speeds GPCR target validation. concerns and regulatory hurdles: Non-radioactive alternative to screening In the context of CNS drug development A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.

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 Cryptic Sites, Longer Onset: Why Some Drugs Work Differently in Cells Than in Assays One of the most This has direct implications for: Assay timing and readout design Misclassification of lead candidates Corner  is your trusted, expert-led guide through the evolving landscape of GPCR science.

GPCR signaling wasn’t linear. It wasn’t clean. Why GPCR Collaboration Is Essential for Modern Science Hodson makes the point bluntly: modern GPCR science metabolic phenotyping facilities for in vivo work, structural experts for cryo-EM, chemists for tool development Together, they push GPCR science faster. signaling in metabolic tissues Using genetics to understand responder vs. non-responder profiles Developing

GPCR internalization assay now featured in the Dr. Developed to address long-standing challenges in GPCR internalization assays , pHSense™ reagents  combine Eric Trinquet, Director of Research and Development at Revvity.   Tool Designed for Real Research Needs s of GPCR assay innovation , pHSense™  was developed to overcome assays  and the scientific “aha” moments that drove its development.

It was supposed to be just a summer project—routine pipetting, repetitive assays, a box to tick before Many GPCR scientists trace their origin story back to a single unexpected spark. Not a grand plan. 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.

Here we developed and validated a label-free, liquid chromatography-mass spectrometry (LC-MS) based cell binding assay can be difficult to achieve. In one example, to study a G protein coupled receptor (GPCR), we used one antagonist as probe and multiple binding affinity was consistent with functional assays. Read more at the source #DrGPCR #GPCR #IndustryNews

Watch Episode 175 From failed assays to breakthroughs in GPCR modeling , Dr. At that point, very few GPCR crystal structures had been determined. Rather than focusing solely on explaining receptor behavior post hoc, his group began developing workflows Carlsson notes that it’s easier to find pharmacologists to run assays than it is to persuade chemists Trainees must learn how to interpret assay data, understand pharmacological context, and communicate

Welcome GPCR Fans,   In GPCR-targeted drug discovery, precision isn’t optional—it’s a requirement. GPCR Premium Members this week gain curated, early access to: Industry insights : GPCRs and mRNA in drug structure-activity relationship (SAR) cycles Wasted optimization efforts Focus on leads that fail later in development Wendy Young : Career insights and lessons from a leader in drug development and a champion for women GPCR Premium Membership Gives You an Edge Dr.