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Radioligands have been used to study GPCRs for decades, but with the advances in the fluorescence field, assays They are ligands labeled with radioactive isotopes which can be used in binding assays to quantify other 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.

Overcoming them requires careful assay design and strategic use of the right fluorescent probes. For GPCR assay developers, HCS supports:  Quantitative visualization of receptor internalization and trafficking  • Live-cell kinetic measurements  unavailable to endpoint assays  Multiplexed assessment the gold standard for image-based GPCR assays. development expertise.

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

Enhance your GPCR research with deeper assay insights for more effective results. 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.

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.

New scaffolds modulating the CBRs in both the orthosteric and allosteric sites have been developed, supported by resolved crystal structures of both CBRs.[4–8] A key challenge in CBR modulator development is separating Results 2.1  CELT-335 Binding at CB1 and CB2 Receptors The first step for the development of the assay Using these results as a starting point, the Tag-lite® binding assay was developed. and the Tag-lite® binding assay developed in this work. ( a ) CB1R binding affinities; ( b ) CB2R binding

Assay volume control does just that. It’s about revealing therapeutic liabilities before  they derail development. The real question: are you letting your assay system dictate the wrong story? between a high-affinity/low-efficacy agonist  versus a high-efficacy agonist  before entering costly development Clarify whether observed effects reflect true pharmacology or assay artifacts .

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 measuring G protein recruitment/activation, inositol phosphate accumulation, or Ca2+ mobilization), assays 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."

physiological processes, making them a key target in drug development.   This technology enhances sensitivity and assay specificity . In a recent study , we contributed to the development of a robust HTRF assay for the discovery of new Saturation assays using CELT-335. By combining deep expertise in GPCR biology with advanced fluorescence chemistry, Celtarys custom-developed

The dysfunction of these receptors has been linked to the development of many serious pathologies, like Thus, developing assays for commercially available probes such as CELT-419 would facilitate research Probe characterization and assay development and validation 3.1  Characterization of CELT-419 in radioligand To validate that the developed assay is suitable for measuring the K i of different ligands, competition Altogether, the development of similar probes for other GPCRs and further development of measurement

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? Built to Fail, Built to Win: The IP One Gamble After the success of their cAMP assay, Trinquet’s team took a risky bet: develop a functional readout for Gq signaling without relying on calcium. Months were spent debating assay design. IP1 isn’t naturally abundant or easy to detect.

Here we developed and validated a label-free, liquid chromatography-mass spectrometry (LC-MS) based cell binding assay, using centrifugation to separate binders from non-binders. This assay was applied to various target classes, with particular emphasis on those for which protein-based binding assay can be difficult to achieve. binding affinity was consistent with functional assays.

Industry insights:  New alliances, pipeline shifts, and platform tech that could reshape metabolic drug development Localization Matters : Protein complexes pre-assemble at membranes, altering how ligands trigger responses. • Assay Development Gets Real : Fluorescent tools and real-world biology don’t always match. University access are coming—grandfather pricing ends in 2026. • Inclusive Growth : More access for developing Whether you’re designing the next assay, scouting a new therapeutic angle, or exploring career pivots

Eric Trinquet Built to Fail, Built to Win: Inside the IP1 Assay Origin Story The IP-One assay didn’t 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 “We did a full dose-response and saw antagonism—all in one plate-based assay. Product development isn’t just about science.

“We don’t just deliver compounds, we solve assay problems.” — Dr. Maria Majellaro Celtarys specializes in the custom development of fluorescent ligands  using a modular Democratize access to high-performance chemical probes and make assay development faster, cheaper, and workflow on the company page . _______________ Keyword Cloud:   GPCR data platform , fluorescent ligands , assay development , GPCR research community , Dr.

offset rates (not just “final numbers”) decide which drugs succeed in patients and which ones die in development kinetics ✅ A framework to classify antagonists and rank compounds by offset rate, using rapid calcium assays The Hemi-Equilibrium Problem Calcium assays look simple. Flip it around, and you’ve got a shortcut: use depression of max in calcium assays to rapidly rank offset The reality is dynamic—ligands arrive, depart, and interact in ways that standard assays often miss.

Does Your Assay Agree With the Literature? Your experiment gives a pKB of 8.0. Is that consistent, or is your assay biased? to: Confirm whether your mean truly overlaps with accepted values Verify if binding and functional assays interchangeable with existing ones Instead of vague comparisons, you’ll have statistical clarity on whether your assay suggestions Practical insights  distilled from decades of pharmacology experience Whether you’re validating assays

August 2022 Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based The GloSensor™ cAMP assay enables real-time monitoring of signaling downstream of many GPCRs. However, it is crucial to optimize assay conditions such as temperature. Here, we describe the temperature sensitivity and reversibility of the GloSensor™ cAMP assay, and which Nevertheless, the GloSensor™ cAMP assay can be applied to analyze signaling by a wide range of GPCRs

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. Mini Timeline: Manual assay years — technical rigor as foundation Technology boom — scaling curiosity

When Sokhom joined Alkermes, the company had a strong development arm, but a relatively underdeveloped tasked with building an in vitro pharmacology group from scratch , including infrastructure, hiring, assay development, and team dynamics.

affinity experiments  are interpreted—and how those interpretations quietly shape SAR, lead selection, and development By walking through saturation curves, displacement assays, stoichiometry pitfalls, and kinetic traps, experiments that tell the truth , ensuring affinity data support—rather than undermine—lead selection and development 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

visibility and adoption of Celtarys’ cutting-edge fluorescent ligand technology and accelerate the development Celtarys Research develops high-quality, fluorescently labeled ligands and innovative chemical biology tools to support real-time, non-radioactive GPCR assays. About Celtarys Research Celtarys Research is a biotech company based in Spain that specializes in the development development, screening, and live-cell imaging.

Someone with strong assay development skills as well as strong data analysis and interpretation skills Mark:  “Are there particular assay types of interest?” Beth:  “We focus on biochemical, cell based, and radioligand binding assays to enable SAR, MOA, lead s comradery and open exchange in our team and I strive to provide learning opportunities for career development

In this session, you’ll gain: Why saturation and displacement assays fail when protein stoichiometry The midpoint and maximum—core parameters for downstream modeling—are only meaningful when the assay fully Displacement Curves and the Illusion of Potency Displacement assays measure affinity when no traceable Equilibration time:  Many assays stop before the system reaches equilibrium, especially with slow competitors

Traditional assays—particularly membrane-based radioligand binding—often provide high-throughput measurements study, 16 synthetic cannabinoid receptor agonists (SCRAs) were evaluated using a CB2 live-cell HCS assay Traditional membrane-based assays isolate receptors from this environment, which simplifies quantification Visual displacement provides an additional confidence layer that traditional homogeneous binding assays or GPCR-mediated analgesia, these findings reinforce the value of physiologically relevant binding assays

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,

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

This conjugation is very useful for tagging biomolecules and can also be used to develop fluorescent Chapter Three - Bioconjugated Materials in the Development of Subunit Vaccines.

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.

GPCR Binders, Drugs, and more Development of a 5-HT7 receptor antibody for the rat: the good, the bad Industry News Data Presented at AACR 2023 Highlights Exscientia’s Clinical and Preclinical Development Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. FREE Symposium - IPI Surfacing (June 15, 2023) Training School on “Cell-based assays to study Adhesion Development Post Doctoral Fellow Research associate in protein production Vice President, Oncology Clinical