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- Understanding Enzyme Inhibition In GPCR Discovery Programs
understanding inhibition to advance GPCR drug discovery This Week’s GPCR Intelligence: Every drug you design Whether you’re designing a ligand, optimizing ADME, or predicting PK, enzyme inhibition defines what This week’s Terry’s Corner reframes inhibition not as background theory—but as a design lens for smarter When “inhibition” becomes activation—and how that insight fuels next-gen therapeutic design. Members-only networking, AMAs & matchmaking 💡 Support open resources for the global GPCR field 🧠Designed
- Terry’s Corner, Celtarys' Leap, and the $7B GPCR Horizon
Whether you’re early in your career or pushing the edge of MoA design, weekly lesson help you apply key Terry Kenakin  Terry’s Corner is your space focused on GPCR pharmacology designed just for you.  With strong signal stability, HTS compatibility, and broad assay versatility, CELT-419 is designed for
- Why Kinetics Matter More Than Kd in GPCR Drug Discovery
. 🔍 This Week in Premium: Sneak Peek A curated preview of this week’s Premium classified content — designed to keep you ahead without noise or delays: Industry insights:  Structure-Based Drug Design Summit; AI-Powered Must-read publications:  GPCRchimeraDB: Database of engineered GPCR designs. lectures, classified industry news, priority event alerts, job opportunities, and insider commentary—all designed GPCR Premium is designed for scientists who need the right intelligence, fast—without noise, distractions
- When the Islet Lit Up: Advancing GPCR Imaging in Native Tissue
How a Chemical Design Sparked a GPCR Imaging Breakthrough The concept was elegant: antibodies weren’t The design didn't just work — it revealed. Interdisciplinary design isn’t optional in GPCR imaging. strategies for parallel receptor mapping Super-resolution imaging of receptor nanodomains AI-assisted probe design
- FDA Approval Is a Strategy Obstacle, Not a Paperwork Problem
And if your development plan was designed to persuade , not to withstand pressure , then you are not This is the principle of strategic reverse engineering . 👉 It means designing your development path in practice: You align trial endpoints with future label claims , not just scientific curiosity You design your leadership team evaluates options. ✅ Every strategic decision, from indication selection to study design It’s to design smarter , from the very beginning.
- Orthosteric vs Allosteric Interactions— and the pHSense Shift in Internalization
Win on kinetics, not just Kd:  Dynamic binding means “affinity” moves—design readouts and decisions that Watch our new trailers for a preview of expert-led GPCR training designed for scientists and drug hunters From Bench Frustrations to Breakthrough Design For decades, GPCR trafficking research relied on overexpression It's designed to help GPCR scientists and teams move faster by consolidating scattered updates into a Members-only networking, AMAs & matchmaking 💡 Support open resources for the global GPCR field 🧠Designed
- From Snapshots to Predictions: Why Mechanism of Action Matters
insights ✅ Tools to distinguish orthosteric vs. allosteric mechanisms ✅ A framework for using models to design They design experiments. In HIV entry studies, purified gp120 was too expensive for routine assays. predictive insights Differentiate orthosteric vs. allosteric mechanisms with confidence Apply models to design It’s learning how to design, interpret, and decide with models built in . Terry’s Corner is designed to give you the edge.
- Assay Volume Control: Your GPCR Drug Discovery Power Lever
Design for translation:  Map sensitivity ranges to tissue contexts so your plate data predicts what happens Watch our new trailers for a preview of expert-led GPCR training designed for scientists and drug hunters But behind every “new” assay is a decade of design, failure, and rethinking. Members-only networking, AMAs & matchmaking 💡 Support open resources for the global GPCR field 🧠Designed
- Accelerating GPCR Drug Discovery: What 40 Years of Pharmacology Reveal
Screening technologies, structure-informed design, and AI are accelerating target selection. Terry’s Corner is designed to shorten that distance between initial promise and actionable clarity. This expands the strategic toolbox for discovery teams: Bias isn’t an “optional property” to design in Weekly lectures  that sharpen your command of how enzyme activity drives pharmacokinetics and drug design
- From Switches to Microcircuits: GPCR Biased Signaling and the Future of Drug Discovery
Ligands designed to activate therapeutically beneficial pathways, while avoiding those associated with side effects, are no longer a theoretical aspiration — they are an active design objective. receptor adopts depends critically on which ligand is bound — a principle now fundamental to rational drug design extensive platform of GPCR functional assays — including β -arrestin, cAMP, and calcium mobilization assays designed
- Dr. GPCR and Celtarys Research Join Forces to Expand Access to Innovative GPCR Tools
dramatically improve how scientists measure ligand-receptor interactions, visualize binding in live cells, and design generation of conjugates, such as labeled ligands, with excellent affinity and pharmacological profiles, designed
- Better GPCR Drug Discovery Decisions Start With Structured Learning
Each piece is designed to help you make better decisions—faster. 🔍 This Week in Premium: Sneak Peek It is operational pharmacology designed to prevent avoidable setbacks. courses and three live AMAs covering binding, kinetics, efficacy, mechanism, ADME, and experimental design
- Unlock the Hidden Complexity Behind GPCRs—From Terry Kenakin’s Vault
It’s 40 years of hard-won insight distilled into accessible, high-impact content designed for learners
- Pharmacology at Your Fingertips: Terry’s Corner Launches
Yamina’s Corner delivers GPCR consulting that cuts through the noise, designing assay cascades, setting chemokines and their receptors drive selectivity and promiscuity, paving the way for rational ligand design
- Dr. GPCR Spotlights Revvity’s pHSense™ Internalization Tools
A GPCR Internalization Tool Designed for Real Research Needs Built on more than two decade A GPCR Internalization Tool Designed for Real Research Needs s of GPCR assay innovation , pHSense™  was developed to overcome
- GPCR Allostery: Unlock Hidden Mechanisms and Make Smarter Drug Decisions
Some drugs take hours to reach equilibrium—not because of poor design, but because the system is fluid Why you need to be there: Learn how kinetic nuance shapes ligand design.  lectures, classified industry news, priority event alerts, job opportunities, and insider commentary—designed
- GPCR Selectivity Beyond the Receptor
Purinergic GPCR Ligand Design: A3AR and P2Y14 in Neuropathic Pain A3AR and P2Y14 represent mechanistically with Kenneth Jacobson and Matteo Pavan examines the structural determinants that make selective ligand design allosteric sites at A3AR operate independently of the orthosteric pocket, with implications for PAM design
- đź“° GPCR Weekly News, February 13 to 19, 2023
GPCR Jobs Computational drug design PhD student at the Department of Drug Design and Pharmacology Computational drug design postdoc at the Department of Drug Design and Pharmacology Software / database development PhD student at Department of Drug Design and Pharmacology Software / database development postdoc at the Department of Drug Design and Pharmacology Postdoc in Bioinformatics/Data Science at Department of Drug Design and Pharmacology Scientist/Senior Scientist (Research Software Engineer) Senior Scientist
- Amylin Receptor Signaling: Three Receptors From One, and How to Profile Each
Three subtypes, three pharmacologies This heteromeric architecture is the reason amylin-directed drug design For a discovery team, that turns subtype identity into a first-order design question. Answering those questions cleanly, and early, is what separates a rationally designed amylin therapeutic
- Breaking the Myth of High and Low Affinity Sites
to decision faster, with fewer false starts  This isn’t textbook material—it’s real-world expertise designed The analytical tools that shaped traditional affinity analysis were designed for simpler systems.
- Do You Believe AI Could Accelerate Drug Discovery?
ability to accurately predict protein structures is transformative for identifying new drug targets and designing The AlphaFold database encompasses over 200 million proteins, aiding structural biology, protein design Furthermore, AI's role in structural biology and drug design is set to spark innovation in automated
- Optimizing HTRF Assays with Fluorescent Ligands: Time-Resolved Fluorescence in GPCR Research
By using donor-acceptor pairs with different emission spectra that don’t overlap, researchers can design This assay utilized our fluorescent ligand, CELT-335 , designed for hCB 1 /CB 2  cannabinoid receptors power of HTRF and other FRET-based technologies by providing high-performance fluorescent ligands designed
- Exclusive Access: Terry's Corner is LIVE + Your Premium Member Discount!
This isn't just another lecture series; it's a practical tool designed to help you recognize and build
- Pepducin-mediated G Protein-Coupled Receptor Signaling in the Cardiovascular System
October 2022 "Pepducins are small-lipidated peptides designed from the intracellular loops of G protein-coupled To date, pepducins designed from numerous GPCRs have been studied for their impact on pathologic conditions This review will focus in particular on pepducins designed from protease-activated receptors, C-X-C motif
- Exscientia is 10 years old this July!
Founded as a spinout from the University of Dundee on 20 July 2012, Exscientia pioneered the design of We have achieved a great deal in the last decade, such as the first-ever AI-designed drug candidates We’re excited about delivering the next ten years of Exscientia and advancing AI to design better drugs
- đź“° GPCR Weekly News, January 30 to February 5, 2023
GPCR Jobs Computational drug design PhD student at the Department of Drug Design and Pharmacology Computational drug design postdoc at the Department of Drug Design and Pharmacology Software / database development PhD student at Department of Drug Design and Pharmacology Software / database development postdoc at the Department of Drug Design and Pharmacology Postdoc in Bioinformatics/Data Science at Department of Drug Design and Pharmacology Scientist/Senior Scientist (Research Software Engineer) Senior Scientist
- Inside the New Dr. GPCR Ecosystem: Learning, Insight, and Momentum for 2026
After a brief pause over the holidays and last month, we’re back in full force—designed to help you make GPCR Premium is designed for scientists and teams who can’t afford to chase every headline—or miss the
- Asking Better Questions in Science: A Practical Guide for Emerging Researchers
Why Asking Better Questions in Science Improves the Work Itself For JB, questions fuel the way he designs In his collaboration with David Hodson, every major leap—from early ligand design to GPCR visualization
- From Pipettes to Platforms: The Evolution of GPCR Research
for what would become the evolution of GPCR research — a transformation that reshaped how scientists design Today, success depends less on manual precision and more on experimental design, data interpretation,
- Lab Leadership Without Ego: How Sokhom Pin Built the Happiest Team at Alkermes
empowerment , not micromanagement He hired based on attitude and team fit , not just credentials He designed



























