. ✅ Practical ways  to integrate kinetics, allostery, and bias into smarter development decisions. ✅ The real friction point lies downstream : translating receptor–ligand interactions into actionable development Early In Vivo Wins the Race When is the right time to move beyond cell assays? How CRO Communication Impacts GPCR Drug Development Success Even the best science falters without operational Direct input  on future sessions—so topics match the hurdles your team faces in discovery and development

December 2021 "Drug development is rarely trivial. typically require years to uncover the mechanisms of disease before they can even dare to contemplate the development Nevertheless, researchers have a host of new technologies at their disposal to develop targeted therapies Modern drug development approaches include a range of techniques leveraging structural biology, immunology

You can have the most brilliant minds and cutting-edge assays, but if your science isn't continuously My work isn't just  about the latest and best assay; it's about the framework that ensures the right assay data leads to the right decision. We'll look at how overlooked operational details, such as misaligned data from diverse GPCR assay types

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 Eric Trinquet, Director of Research and Development at Revvity.   innovation , pHSense™  was developed to overcome three persistent barriers in internalization studies  and the scientific “aha” moments that drove its development.

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 FP assays are convenient and easy to manipulate. polarization technology is expected to expand its role in GPCR research through the development of novel

A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties We review the current state of CB2 ligand development and progress in optimising physicochemical properties

A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties We review the current state of CB2 ligand development and progress in optimizing physicochemical properties

Today, InterAx Biotech is pleased to announce that Carola Weiss has joined the company as VP Business Development Carola Weiss’ professional career brings deep expertise in business development, marketing & sales, licensing

(Nasdaq: TRVN), a biopharmaceutical company focused on the development and commercialization of novel patients with central nervous system (CNS) disorders, today announced it is advancing TRV045 into clinical development TRV045 is the Company’s novel S1P1 receptor modulator being developed as a potential treatment for diabetic

a set of 7 cannabinoid ligands (both natural and synthetic) to validate and optimize the assay. Because Tag-lite® is based on FRET, we have collaborated with BMG Labtech to develop an application note 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.

It was simply a clean, scalable assay—and a wave of new possibilities. That’s the promise of pHSense, a groundbreaking reagent developed by Eric Trinquet and his team at Revvity This was the foundation of a new set of assay tools. Mini Timeline: pHSense Development Early 2020s: Rare-earth probe synthesis begins Collaborative screening User feedback will guide the development of future tags and variants.

fibrosis, cancers, cardiovascular diseases and neuropathic pain, making it a promising target for drug development This article provides an extensive review on the current status of ligand development targeting LPA receptors

January 2022 Exscientia and Sanofi Establish Strategic Research Collaboration to Develop AI-driven Pipeline Sanofi and Exscientia announced today a groundbreaking research collaboration and license agreement to develop

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 Introducing Celtarys - Probe Development via Conjugation Strategies   Celtarys Research's first article provides a detailed examination of conjugation strategies to develop high-performance fluorescent probes It emphasizes scaffold selection, linker optimization, and assay compatibility to enhance target binding

medicinal chemistry paved the way to co-founding Celtarys , a company now shaping the future of GPCR assay Over time, she developed a fascination with how molecules influence biology and how that chemistry could The academic group Maria worked with had developed a technology that allowed for flexible, fast synthesis GPCR, is helping researchers worldwide gain access to customized, reliable assay tools without the delays and frustrations that often plague probe development. 👉 Learn more about Celtarys’ science-driven solutions

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

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 go/no-go points, and de-risking programs from hit validation through development candidate selection 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. 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 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

June 2022 "We’re delighted to welcome Dr Ed Brennan as our new Vice President, Head of Clinical Development Dr Brennan has extensive experience across all phases of clinical development, and across multiple therapeutic

December 2022 Sosei Heptares Enters Antibody Discovery Agreement with Twist Bioscience to Discover and Develop (“the Company”; TSE: 4565), the world leader in GPCR-focused structure-based drug design (SBDD) and development

November 2021 Twist Bioscience Launches Revelar Biotherapeutics to Develop and Commercialize Novel COVID Executive Leadership Team Established with Demonstrated Success in Clinical, Regulatory and Commercial Development has launched Revelar Biotherapeutics, Inc., an independently operated, new biotechnology company to develop

empowers scientists to simplify complex workflows, accelerate discovery, and drive breakthroughs in drug development The first company to offer access to recombinant GPCR assays. Today, their catalogue includes over 1,000 functional assays representing more than 550 GPCR and other targets, trusted by therapeutic developers worldwide for affinity, potency, efficacy, and functional Their platform delivers kinetic profiles that reliably inform decisions and reduce the risk and cost of developing

(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. pharmacological activity, allowing for the determination of drug kinetics—a critical aspect in drug development Some innovative solutions have been the development of the BERKY and the ONE-GO biosensors, designed

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

Corner, Yamina's Corner, biotech, systems thinking, signal transduction, operational excellence, drug development

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

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.

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