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- A robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.
This can be appreciated when talking about SCRAs (Synthetic Cannabinoid Agonists), as one of the series It has been applied to different GPCR binding assays, such as CXCR4, opioid receptors, CCK1 and CCK2. In the saturation experiments, specific binding was also checked, employing appropriate competitors ( Time-Resolved Detection of Energy Transfer: Theory and Application to Immunoassays. Principles and Biophysical Applications of Lanthanide-Based Probes.
- Radioligands vs. Fluorescent Ligands: Binding Assays
for decades, but with the advances in the fluorescence field, assays have shifted towards fluorescent-approaches This is complimentary with other applications, and essential in our understanding of signaling pathways
- Fluorescence based HTS compatible ligand binding assays for dopamine D3 receptors in baculovirus preparations and live cells
pathologies, like depression, schizophrenia and Parkinson’s disease. [1,2] Several dopamine ligands have been approved ± SEM value for CELT-419 binding to D3 receptor was determined to be 30.1 ± 1.7 nM corresponding to apparent Miniaturization is key for HTS application, so achieving good Z’ values for GPCR ligand binding assays
- Conjugation Strategies for Probe Development
Not only do they work in aqueous medium, but also in aprotic solvents like DMF, where you will need to
- Is Your GPCR Drug Discovery Program Built for Breakthroughs or Breakdowns?
This reactive approach, driven by a "go fast" mindset, burns through precious capital and time, leaving This reactive approach, driven by the prevailing wisdom of "going fast" and focusing only on the science This simple truth applies profoundly to the "go fast" culture in biotech. I understand that embracing a systematic approach can feel daunting, especially with the pressure to It's the opposite of a reactive approach, where problems are solved in isolation.
- Target Residence Time: The Hidden Driver of In Vivo Efficacy
PK–PD Dissociation: When Clearance Doesn’t Mean It’s Over The lecture’s standout example: Aplaviroc,
- Competitive vs Non-Competitive GPCR Antagonists: How to Interpret Pharmacology Data with Confidence
Solve the problem of a fragmented approach by learning how to build a unified system where every scientific This event is a critical opportunity to stay informed, but the real advantage lies in applying these content is meticulously vetted and organized to provide clarity and actionable insights that you can apply
- Breaking the Myth of High and Low Affinity Sites
In this session, you’ll gain: ✅ A framework for understanding when apparent multiple affinities really Every day spent misunderstanding the meaning of apparent affinity differences can slow your project’s At first glance, when a ligand appears to bind at two different affinities in the same system, it seems It’s common to observe two apparent affinities for a ligand under certain experimental conditions. In many systems, a ligand may appear to bind with very high affinity when it facilitates formation of
- How Fast Does a Drug Work?
Without appreciating their limitations, it’s easy to misinterpret key kinetic signals that matter for
- Are You Guessing or Forecasting? Master GPCR Pharmacologic Models Before It’s Too Late
Break stagnation: Apply lessons from BMS, Novartis, Cerevel & more.
- Your GPCR Program Decisions Depend on Good Data Interpretation
structural insights into peptide ligand activation All curated for speed, relevance, and immediate application—only Under certain experimental conditions, what appears to be a second high-affinity site may simply reflect Every day spent misunderstanding apparent affinity differences delays key milestones. 🗣️ “Thank you curiosity-driven research Support work-life balance without compromising scientific excellence His approach
- GPCR Allostery: Unlock Hidden Mechanisms and Make Smarter Drug Decisions
publications: CXCL12 dimer impact on AML migration, mechanosensitive behavior in GPCRs, and in vivo APLNR
- How Understanding Intracellular Drug Access Can Transform Your GPCR Drug Discovery Program
To succeed, you need to move beyond standard approaches and adopt the frameworks that are driving real
- Building Backwards: Why Top-Down Models Could Revolutionize Pain Research
Alex Serafini explains, this conventional bottom-up approach often fails to deliver therapies that truly This approach reflects his focus on developing models that behave like patients before molecular exploration This patient-centric and behavior-first approach uncovered robust gene expression signatures linked Why This Approach Matters In pain research, bottom-up approaches often fail to translate. Drugs that look great in vitro fall apart in humans.
- Why Kinetics Matter More Than Kd in GPCR Drug Discovery
All curated for speed, relevance, and immediate application—only for Premium Members.
- Understanding Orthosteric Binding: The Key to Drug Action
This understanding can enhance your appreciation for drug development and therapeutic action. Understanding the intricate details of drug-receptor interactions transforms how we approach pharmacology
- Accelerating GPCR Drug Discovery
My Approach: Biology, Execution, Systems My consulting approach uniquely blends deep pharmacology expertise
- From Technician to Trailblazer: How Sokhom Pin Designed His Own PhD Program While Working in Industry
for presentations All research was publication-quality, high-impact, and strategically focused This approach
- Why Dose-Response Curves Are Pharmacology’s Secret Weapon
statistical tricks that elevate a rough curve into a real insight You'll leave with practical tools and a new appreciation
- Unlock the Hidden Complexity Behind GPCRs—From Terry Kenakin’s Vault
Join Terry’s Corner and stay updated on the latest in GPCR research—delivered in a format that’s as approachable
- Beyond the Probe: Scaling Innovation From the Bench to Product Launch
But what sets them apart isn’t just chemistry. It’s empathy.
- 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 bias, kinetics, and core models—fundamentals that fuel confidence and fluency Move beyond theory to apply GPCR Podcast appearance. Read how scientific need and timing drove the leap from academia to application. oligomerization sustains oncogenic signaling in lymphoid neoplasms, and its disruption boosts sensitivity to the apoptosis-inducing
- From Lab Bench to Boardroom: The Unexpected Path of a Medicinal Chemist
time, she developed a fascination with how molecules influence biology and how that chemistry could be applied
- From One to Many: How a GPCR Curiosity Became a Field-Wide Toolkit
Why It Matters This isn’t just a dataset, it’s a shift in how GPCR biology is approached : Study known
- Ben Clements on Rescuing Opioids with GPCR Modulators
Ben’s approach injects new life into an area most clinicians have given up on.
- Mapping Motion: Intermediate States, Deorphanization & Discovery
A powerful three-color approach captures dynamic receptor states in real time.
- The Perils and Guardrails of Modifying Signalling Proteins in Bioassays
1-4] that requires $1–2 billion [5-8] invested over 10–15 years [5, 9, 10] with only a 7% chance of approval Practical approaches to evaluating and optimizing brain exposure in early drug discovery. Approval success rates of drug candidates based on target, action, modality, application, and their combinations Allostery in Its Many Disguises: From Theory to Applications. Quantitative approaches for studying G protein-coupled receptor signalling and pharmacology.
- 🎄 Have Yourself a Merry Little GPCRmas! ❄ Dec 9 - 15, 2024
GPCR, we believe the same principle applies to building a better experience for our online community | PepTalk 2025 January 25 - 29, 2025 | SLAS 2025 February 15 - 16, 2025 | Structural and Functional Approaches Discovery March 12 - 14, 2025 | NextGen Biomed 2025 March 25 - 28, 2025 | 10th German Pharm-Tox Summit April 1 - 5, 2025 | XXIII GEM Meeting in 2025 April 3 - 6, 2025 | ASPET 2025 April 14 - 17, 2025 | 20th Drug Discovery Chemistry April 24 - 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR
- GPCR News Flash! Top Updates You Can't-Miss! + University CheatSheet is finally available! ❄ Dec 2 - 8, 2024
| PepTalk 2025 January 25 - 29, 2025 | SLAS 2025 February 15 - 16, 2025 | Structural and Functional Approaches February 15 - 19, 2025 | BPS 2025 February 16 - 21, 2025 | Harnessing the Power of Advanced Multimodal Approaches Discovery March 12 - 14, 2025 | NextGen Biomed 2025 March 25 - 28, 2025 | 10th German Pharm-Tox Summit April 1 - 5, 2025 | XXIII GEM Meeting in 2025 April 3 - 6, 2025 | ASPET 2025 April 14 - 17, 2025 | 20th Drug Discovery Chemistry April 24 - 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR
- Hop in the Time Machine with GPCR: Unraveling the Future of Research! ⦿ Nov 24 - Dec 1, 2024
A with Sean McClain, Founder & CEO, and Zach Jonasson, CFO & CBO at Absci Octant: A Next Generation Approach | PepTalk 2025 January 25 - 29, 2025 | SLAS 2025 February 15 - 16, 2025 | Structural and Functional Approaches Discovery March 12 - 14, 2025 | NextGen Biomed 2025 March 25 - 28, 2025 | 10th German Pharm-Tox Summit April 1 - 5, 2025 | XXIII GEM Meeting in 2025 April 3 - 6, 2025 | ASPET 2025 April 14 - 17, 2025 | 20th Drug Discovery Chemistry April 24 - 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR






























