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- New Tools, Smart Signals, and The Kenakin Brief
On the industry side, Novo Nordisk, Septerna, and Deep Apple advance billion-dollar GPCR programs, while linker optimization, and assay compatibility to enhance target binding and signal fidelity in GPCR applications
- Understanding Enzyme Inhibition In GPCR Discovery Programs
Read the Feature ➤ Summer Days: Appetite, Suntans, and GPCR Micro-Domains Two recent papers connect ciliary This spotlight from Montana Molecular dives into how OPN3’s modulation of MCR4 in appetite circuits and
- Enzyme Inhibition Pharmacology: The Hidden Gatekeepers of GPCR Drug Discovery
The same compound may appear inactive in one substrate system, then wildly active in another.
- The Truth About GPCR Product Launches: Years in the Making
Initially applied to biomarkers in blood, its no-wash, miniaturized design caught the attention of high-throughput with Durham University (chemistry) → Discovery of pH-sensitive dual response (brightness + lifetime) → Application
- Assay Sensitivity: The Hidden Lever Driving GPCR Drug Discovery
Questions That Make or Break a Program This session doesn’t overwhelm with technical deep-dives—it teases apart Decades of insight distilled into frameworks you can apply immediately.
- Orthosteric vs Allosteric Interactions— and the pHSense Shift in Internalization
Read fast, apply faster, and stay ahead in GPCR drug discovery with evidence-based insights—no hype,
- Orthosteric vs. Allosteric Interactions: The Silent Decider of Safety and Success
teams navigating safety margins, biased signaling, and combination therapy design, understanding which approach so the content tracks your team’s challenges Decades of insight distilled into frameworks you can apply
- Optimizing HTRF Assays with Fluorescent Ligands: Time-Resolved Fluorescence in GPCR Research
bound to is promiscuous, it will not compromise assay integrity the same way it would in single-label approaches Examples of HTRF donor/acceptor pairs Expanding Time-Resolved Fluorescence Applications in Drug Discovery Beyond Traditional Methods At Celtarys, we have expertise in time-resolved fluorescence applications HTRF: A technology tailored for drug discovery - a review of theoretical aspects and recent applications
- Targeting GPCRs in the CNS: Advances in Drug Discovery Strategies
Over 30% of FDA-approved drugs target GPCRs, with many targeting CNS located GPCRs. Orphan GPCRs in Neurodegenerative Disorders: Integrating Structural Biology and Drug Discovery Approaches Orphan GPCRs in Neurodegenerative Disorders: Integrating Structural Biology and Drug Discovery Approaches
- How to Design GPCR Drugs That Work in Vivo: Strategy, Tools, and Insights
Innovative design approach emphasizing scientific principles over speculation. Upcoming events: 47th Symposium on Hormones & Cell Regulation; new approach to GPCR internalization the podcast ➤ Celtarys Research – Optimizing HTRF with Fluorescent Ligands Traditional ligand-binding approaches
- Why Opposing Processes Matter for Your Next GPCR Drug
Ghrelin receptors, for example, signal spontaneously, meaning a neutral antagonist won’t suppress appetite
- Dr. GPCR Spotlights Revvity’s pHSense™ Internalization Tools
GPCR Podcast , where he shares the story behind pHSense , including its application in real-time internalization
- How Advanced GPCR Kinetics Sharpen Decision Making (and Save You Time)
into cholesterol interactions in the active conformation of GLP‑1 receptor Terry's Corner – Advanced Applications Out-decide your competition: Apply fractal potency insights to prioritize leads that stay robust across
- GPCR Drug Discovery at Discovery on Target: Why This Track Is About More Than Receptors
Push the boundaries of receptor pharmacology and its real-world applications. Kenakin breaks down receptor pharmacology, functional selectivity, and ligand bias in a way you can apply
- The Five Traps of Ignoring Kinetics
Unlock “Kinetics: Advanced Applications” Only in Terry’s Corner Why Terry’s Corner Most pharmacology
- Mechanism vs. Assumption: A Model-First Path to Getting GPCR MoA Right
You’ll apply a model-first workflow to classify orthosteric vs. allosteric behavior, stress-test assumptions This applied article walks through ligand-directed labeling, SNAP/Halo tags, and fluorescent ligands
- Integrating Fluorescent Ligands into Flow Cytometry: Enhancing GPCR Analysis Beyond Traditional Antibody Staining
. - High-throughput applications Bright and stable fluorescent ligands can be used in HTS, Fluorescent ligands are an advancement for flow cytometry applications in the GPCR field, as they overcome
- From Snapshots to Predictions: Why Mechanism of Action Matters
They take descriptive data from one system and translate it into parameters that can be applied to others Without the right model, it’s like staring at identical twins—you can’t tell them apart until you see snapshots into predictive insights Differentiate orthosteric vs. allosteric mechanisms with confidence Apply It’s a shift in how you approach discovery.
- How a Failed Med School Dream Sparked a GPCR Biotech Revolution
His work spans deep academic research, startup life, and the application of machine learning and pharmacology The company’s scientific approach relied on targeting GPCRs — specifically opioid receptors — using biased
- How to Use Statistical Methods to Strengthen Every GPCR Drug Discovery Decision
Eliminate subjective calls: From t-tests to ANOVA and F-tests, know which tool to apply when, so debates
- GPCR Happy Hour – Boston, Sept 2025
This comprehensive approach enables Axxam to support clients worldwide in identifying and optimizing
- Curve Shifts Don’t Lie, But Your Eyes Might
It’s a shift in how you approach discovery. And once you make that shift, you’ll never go back.
- Understanding the Journey: Catherine Demery's Path to Addiction Science
She found herself drawn toward the science behind the drugs, rather than their clinical application. “It really forced me to kind of patch up all my immunology holes and then apply them. I came away from that job with just a whole new appreciation for immunology and for pregnancy.
- Purpose-Driven Opioid Research: Catherine Demery’s Academic Path
This approach makes her models not just rigorous, but translational—bridging the gap between receptor
- The Hidden Driver of GPCR Drug Success: Why Target Residence Time Matters More Than You Think
targeting obesity to significant collaborations in cardiometabolic disease, and gain insights into novel approaches
- Fluorescence Polarization in GPCR Research
How Fluorescence Polarization Assays Work: Principles and Applications in GPCR Research FP assays work Target-based drug discovery: Applications of fluorescence techniques in high throughput and fragment-based
- Fentanyl and Xylazine: Why Breathing Fails in Overdose
combination is not merely additive; it’s synergistic, shrinking tidal volume even when breathing rate appears The real killer, however, is apnea—those silent pauses where oxygen saturation crashes, often missed With fentanyl, the danger lies in apneas —complete pauses in breathing. Even if the respiratory rate doesn’t appear drastically lower, those pauses send oxygen levels plummeting A patient might appear stable on an oxygen monitor, even as their breathing mechanics are deteriorating
- Why “Displacement” Misleads You: Allosteric Binding Demystified
If you’re applying orthosteric logic to modulator-driven systems, you’re likely misreading your assays—and
- Advantages of Fluorescent Probes in GPCR Assays
challenge in drug discovery: a vast therapeutic potential with many targets yet to be explored. 35% of FDA-approved The fluorescence plateaus after approximately 10minutes. It can be appreciated how fast the ligand diffuses and is distributed homogeneously within monolayers , staining both apicobasal and lateral membranes (Figure 1B). Fluorescent approaches for understanding interactions of ligands with G protein coupled receptors.
- Differential binding of Δ9-tetrahydrocannabinol derivatives to type 1 cannabinoid receptors (CB1)
Because Tag-lite® is based on FRET, we have collaborated with BMG Labtech to develop an application note They regulate mood, memory, appetite and motor function. If you want to check out the Materials and Methods section as well as the application note, here is the






























