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. • Assay Development Gets Real : Fluorescent tools and real-world biology don’t always match. Whether you’re designing the next assay, scouting a new therapeutic angle, or exploring career pivots

Functional assays can suggest clarity while quietly masking complexity, creating the illusion of competitive Each experimental decision — system sensitivity, assay configuration, kinetic design — carries strategic Assay Sensitivity and System Configuration Receptor expression level is a strategic variable. Best Habits for Data Quality and Reproducibility Detection assays identify activity; they do not validate promising hits into mechanistic evaluation quickly Use statistics to arbitrate interpretation Design assays

thrilled to have entered a strategic partnership with Eurofins DiscoverX , a global provider of GPCR assay This partnership connects advanced assay and biology capabilities with the scientists and organizations Why this deserves attention: Assay breadth matters.  Platform selection shapes interpretation.

A new NanoBRET® competitive binding assay 2  was developed in collaboration with Professor Kevin Pfleger Scheme of a competitive NanoBRET® assay. GPCRs are part of Celtarys’ expertise fields. The competitive assay design and optimization were performed in the University of Western Australia. The competitive assay design and optimization were performed in the University of Western Australia. First, saturation binding assays were performed .

Must-read publications: D2 receptor constitutively active mutants; β2AR allosteric SERS assay; CXCR4 Start learning here ➤ Terry’s Corner — Early Safety Assays For Better GPCR Drug Discovery Decisions Too Terry Kenakin walks through the core early assays that protect your chemistry, budget, and timeline.

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

These assays offer a simple approach to the comparison of agonist profiles across different pathways For example, Figure 1 shows cell-based assay results from the cAMP G protein activation pathway and the Both assays provide unique profiles and a preferred receptor signaling bias for the therapeutics tested when tested in orthogonal functional assays. Without multi-pathway assays, selectivity assessments can be misleading.

Patient derived iPSC's, organoid systems, and biosensor-based assays introduce models that better preserve cover how patient-derived induced pluripotent stem cells (iPSCs), organoid systems, and biosensor-based assays signaling, producing a fundamentally different pharmacological pattern — with different consequences for assay

Achieving that objective demands assays that can actually see the difference.  GPCR Assay Strategy: Why Binding Studies Alone Miss Biased Signaling Binding assays remain useful as The appropriate response is a multi-assay strategy. No single assay captures the full signaling profile of a GPCR-ligand pair. It also requires alignment between in vitro   GPCR assay  data and pharmacokinetic measurements.

October 2022 "We describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR) for 19F-NMR and single-molecule fluorescence (SMF) spectroscopy. We explain in detail steps shared between the two sample preparation strategies, including expression and isolation of A2AAR and assembly of A2AAR in lipid nanodiscs and procedures for incorporation of either 19F-NMR or fluorescence probes. Protocols for SMF experiments include sample setup, data acquisition, data processing, and error analysis. For complete details on the use and execution of this protocol, please refer to Wei et al. (2022) and Sušac et al. (2018)." Read more at the source #DrGPCR #GPCR #IndustryNews

pHSense™ reagents enable real-time GPCR internalization detection A breakthrough GPCR internalization assay Developed to address long-standing challenges in GPCR internalization assays , pHSense™ reagents  combine Built on more than two decade A GPCR Internalization Tool Designed for Real Research Needs s of GPCR assay assays β-arrestin recruitment assays Downstream readouts  – phospho-ERK, AKT, CREB, MEK and other phoshoproteins , where he shares the story behind pHSense , including its application in real-time internalization assays

However, these conventional assays often provide limited information on intermediate signaling events (e.g G protein recruitment assay [6], mini-G recruitment assay [7], GRK and β-arrestin recruitment assays [8]), G protein activation (e.g TRUPATH assay [9]), receptor trafficking ( e.g FYVE assay [10]),  β-arrestin  YEN assay [13]), among others. Zhou, Y., et al., Multiple GPCR Functional Assays Based on Resonance Energy Transfer Sensors. 

To efficiently run these screening campaigns high throughput screening assays are used. How Fluorescence Polarization Assays Work: Principles and Applications in GPCR Research FP assays work FP assays are convenient and easy to manipulate. where they used CELT-419 for D3 dopamine receptor binding assays in baculoviruses. 3.       The future of fluorescence polarization assays is closely tied to fluorescent ligands.

During that project we tested its validity as a fluorescent probe for Tag-lite® assays, where we used a set of 7 cannabinoid ligands (both natural and synthetic) to validate and optimize the assay. It bears a hydrophilic fluorophore compatible with the terbium donor in TR-FRET assays. Figure 2.Assay Principle: TR-FRET assay using CELT-335, a dual (CB1/CB2) fluorescent ligand that serves Comparison of binding affi nities using radioligand binding or TR-FRET assays.

Signaling and Translation Heterologous systems such as HEK293 cells enable scalable pharmacological assays Terry Hébert will examine how iPSC-derived cardiomyocytes , organoid systems , and biosensor-based assays Biosensor-based assays enable direct measurement of signaling dynamics within complex biological systems Reserve your spot ➤ GPCR Pharmacology: Open Problems and Discussion Binding assays and functional assays limitation: binding measures the receptor population that engages tracer ligands, while functional assays

It was simply a clean, scalable assay—and a wave of new possibilities. Instead of creating another black-box assay, they designed pHSense around rare-earth europium probes. This was the foundation of a new set of assay tools. Whether in industry or academia, whether overexpressing or not, you can adapt the assay to your system Build or adopt assays that can evolve with your questions—like pHSense.” What’s Next?

programs don’t fail because of weak molecules—they fail because biology behaves differently than the assay His work shows why chemical design can outperform antibodies and how rigorous assay validation bridges But HCS only works when assays are built with rigor and powered by the right fluorescent ligands. What You’ll Learn Why traditional radioligand assays miss critical spatial and kinetic signals Five phases a robust, reproducible HCS pipeline How fluorescent ligands strengthen specificity, relevance, and assay

Docking scores were meaningless without assays. For receptor assays and the biological interpretation of ligands, he relies on a network of collaborators Chemistry fuels assays. Assay data flows back into models. A pharmacologist who understands docking, or a modeler who knows assay constraints, will collaborate , and assay data cycling back to refine predictions.

This framework shaped how assays were designed, how drug candidates were profiled, and how efficacy was BRET-based assays can quantify beta-arrestin recruitment and, depending on the assay design, distinguish Measuring GPCR Internalization: Assay Strategies Beyond Imaging The classical approach to detecting internalization Standard assays capture the initial step, but the frameworks that connect internalization to recycling Terry Kenakin’s session on measuring GPCR internalization walks through the assay logic, the mechanistic

“We don’t just deliver compounds, we solve assay problems.” — Dr. 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

Early assays prevent late failure  — modern in vitro tools dramatically reduce attrition . GPCR Podcast—GPCR Assay Strategy, Bias, and Translational Drug Discovery In this episode of the Dr. Martin Marro shares hard-earned lessons from the interface of assays, bias, and translation. The conversation moves beyond theory into real-world tradeoffs: fluorescence-based assays, internalization Listeners will gain perspective on: Assay choice as strategy , not convenience.

Plus, Celtarys explores ligand selection for better assays, and co-founder Dr. Radioligands – Assay Smarter Celtarys explores how fluorescent ligands enable safer, high-throughput Learn how these tools help retain assay integrity while eliminating radioactivity—perfect for next-gen Maria Majellaro reveals how Celtarys evolved from a vision into a company solving real-world assay problems

Using Fluorescent Ligands Over Antibodies in Flow Cytometry Assays: Key Advantages These are key limitations These limitations can impact data quality, reproducibility, and assay flexibility. Selection for GPCR-Targeted Flow Cytometry The fluorophore tag is a key part of the flow cytometry assay Tag brightness and stability:  the brighter and more stable the better the assay outcome. 2.       CELT-240 in flow cytometry binding assays is suitable to measure the affinity of compounds for the D2

Yamina’s Corner opens for strategic consulting, and our partner Celtarys unveils a robust TR-FRET assay Yamina’s Corner delivers GPCR consulting that cuts through the noise, designing assay cascades, setting Visit Yamina’s Corner Now CELT-335 - Celtarys Validates New Assay for CB1/CB2 Screening Dr. GPCR partner Celtarys Research has validated a TR-FRET assay for cannabinoid receptor ligands using their

Celtarys Research expands its assay tools with CELT-419 for D3 receptor studies, and Dr. translational PK/PD   Subscribe to The Kenakin Brief Fluorescent Probe CELT-419 Powers D3R Binding Assays Celtarys Research presents CELT-419, a nanomolar-affinity fluorescent ligand optimized for D3 receptor assays With strong signal stability, HTS compatibility, and broad assay versatility, CELT-419 is designed for

Maria Majellaro, highlighting their fluorescent ligand tools for live-cell GPCR assays.   Maria Majellaro of Celtarys shares how her team translates medicinal chemistry into practical GPCR assay It emphasizes scaffold selection, linker optimization, and assay compatibility to enhance target binding

Gs protein in complex with the β2-adrenergic receptor (β2AR) at brief sequential intervals following GTP this pathway provide a high-resolution description of the events driving G protein activation upon GTP This interaction significantly increases the receptor’s affinity for GTP, allowing a detailed observation From the initial GTP binding, the structures highlight critical shifts in the α5 helix and the α-helical As GTP stabilizes and migrates towards the P loop, it causes the TCAT motif to shift, a key movement

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 – Precision Tools for GPCR Assays Dr. GPCR and Celtarys Research have teamed up. Sakmar Lab’s Toolkit Goes Public The latest podcast features a discussion about a scalable GPCR-RAMP assay

Corner you'll learn how model-based thinking helps you determine a drug’s mechanism of action and turn assay most difficult calls in pharmacology happen when two different mechanisms look identical in a single assay Without a framework, this looks like an assay error. In HIV entry studies, purified gp120 was too expensive for routine assays. A Case That Seemed Impossible In one real program, a compound produced four completely different assay