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Catch subtle mechanistic drift.   GPCR is a nonprofit organization , and Premium Membership directly supports our mission to make reliable University content, and an integrated view of publications, events, insights, and opportunities designed to support

programs This design had a strategic effect : talent density increased, but so did interdisciplinary surface Suddenly, we could do experiments that individual labs just couldn’t afford. But luck alone doesn’t sustain an ecosystem.

Suddenly, questions that were too risky or expensive to ask in the “manual era” became accessible. Today, success depends less on manual precision and more on experimental design, data interpretation,

It was supposed to be just a summer project—routine pipetting, repetitive assays, a box to tick before Yet that summer research placement cracked open a new reality: the thrill of asking questions no one She moved from “What am I supposed to do?” to “What happens if I try this?” It might be quiet, subtle—an idea you can’t stop thinking about. Pay attention to that. For young scientists, that summer moment is waiting.

Upcoming events:  Global GPCR summits and pharmacology forums shaping 2026 priorities. spatial GPCR signaling shifts discovery—and how leadership, mentorship, and vision shape translational success GPCR evolved from a grassroots effort to a global force in GPCR science—one rooted in connection, sustainability

Opium, for example, was used for dysentery and relief of suffering as early as the 3rd century BC; its Diuretic action discovered in sulfanilamide derivatives led to furosemide; sedative effects of early What matters now is not the category , but the fit: Does the chemical matter support the therapeutic Subscribers gain weekly lectures led by Dr. next decade trying to understand. 40 years of expertise at your fingertips: Explore the full library ➤ Subscribe

This year, we focused on building for sustainability  — strengthening operations, expanding partnerships GPCR stronger, more connected, and more capable of supporting our growing community. We’re continuing to seek new strategic partners  who share our goal of supporting the GPCR community GPCR is evolving — thoughtfully, inclusively, and sustainably.

Suddenly, computational shortcuts weren’t enough. In his view, collaboration is not a bonus or an optional supplement—it is the only way GPCR drug discovery Supporting them is a medicinal chemist who can design and synthesize new scaffolds when commercial libraries If docking can suggest binding modes but can’t resolve nanomolar potency differences, they say so. Biased signaling, allosteric binding sites, and subtype selectivity mean there is rarely a straight line

such as differentiating agonists from antagonists, predicting biased agonism, or achieving receptor subtype For Carlsson, a prediction is only valid if it survives wet-lab testing.   If a method can’t resolve subtle potency differences, the team prefers to acknowledge that limitation But success depends on researchers who can manage expectations, build trust, and integrate across disciplines

A well-behaved molecule in a dish can fail spectacularly in vivo, leaving teams with years of sunk costs How CRO Communication Impacts GPCR Drug Development Success Even the best science falters without operational For scientists in discovery, this means two things: Technical clarity drives survival. Subscribe to The Kenakin Brief  today ➤

Logo Contest : Let your creativity shine by submitting your design for the Logo Contest before August AbbVie Completes Acquisition of Cerevel Therapeutics Nxera Pharma attended the Drug Discovery Ecosystem Summit

When he first began working in a lab, success seemed elusive: experiments often failed, and bench work A summer spent purifying proteins highlighted his discomfort at the bench. His introduction came through a practical suggestion: explore a new protein family that was gaining traction This success was a revelation—it was possible not only to interpret experimental data but to forecast He believes genuine interest—not trends or external validation—is what sustains long-term scientific

framework to predict duration, penetration, and PK/PD separation—so decisions move faster and risks surface Breakthroughs this week:  nanomedicines targeting PAR2 for sustained analgesia; Emerging Voices in GPCR Upcoming events:  Membrane-mimetic screening; GPCR Forum 2025; GPCR-TDD Summit Europe. If your team is designing covalent or tight-binding candidates, these principles reduce surprises and 🗞️ Weekly research, careers & event intelligence 🤝 Members-only networking, AMAs & matchmaking 💡 Support

Watch Episode 174 You never forget the day your data surprises you—in a positive way. For Dr. Eric Trinquet, that moment arrived when his team successfully tracked GPCR internalization in native This success was not mere luck. It’s a subtle yet powerful innovation. These were not mere vendor-supplier relationships.

27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit

27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit Precursor Cells Derived from Patients Diagnosed with Schizophrenia Sphingosine 1-phosphate receptor subtype

This is the silent advantage of many successful drugs: they bind tightly or covalently , making target But it also means new liability surfaces : persistent effects can’t be simply “washed out” when things Subscribe to The Kenakin Brief  today ➤

You can already explore the platform and subscribe to The Kenakin Brief—our new newsletter packed with MOR-positive allosteric modulator (BMS-986122) selectively enhances opioid signaling  through specific Gα subtypes

the mindset that helped shape products used across biotech and academia—and why play, failure, and surprise This mindset, he argues, suffocates innovation. He knows the cost firsthand. For Early-Career Scientists: Don’t confuse “final product” with overnight success.

If you want your molecules to survive first contact with biology, enzyme inhibition must be part of your Breakthroughs this week:  Potentiation of GPCR signaling by ATP and sugar monophosphates; Pharmacology Whether you’re designing a ligand, optimizing ADME, or predicting PK, enzyme inhibition defines what survives Whether you’re building assays or a scientific career, this is a must-read on why risk, surprise, and Read the Feature ➤ Summer Days: Appetite, Suntans, and GPCR Micro-Domains Two recent papers connect ciliary

Enzymes decide who survives. to clinical success. Their broad substrate tolerance shields us from xenobiotics. isn’t a checkbox; it’s a survival test. Subscribe to The Kenakin Brief  today ➤

unlocks a simple lever that separates signal from storytelling, moving programs forward with fewer surprises discovery Flexible , on-demand lessons for busy scientists Influence   the curriculum with your topic suggestions 🗞️ Weekly research, careers & event intelligence 🤝 Members-only networking, AMAs & matchmaking 💡 Support

Built to Fail, Built to Win: The IP One Gamble After the success of their cAMP assay, Trinquet’s team on the front lines of GPCR science, it’s a new lens to see what’s always been there—just below the surface

For drug hunters working at the GPCR interface, the difference between a successful lead and a dead-end Better Predictions For drug discovery scientists, time and predictive accuracy are the currency of success pipeline translates directly into better prioritization, cleaner data packages, and fewer late-stage surprises Unlock Assay Volume Control Only in Terry’s Corner 🎬 Watch Course Trailers Not sure yet? Subscribe to The Kenakin Brief  today ➤

Breakthroughs this week: New work clarifies how active-state GPCR conformations can support coupling GPCR internalization and soluble proteins; core meetings from GPCR Forum to Biophysics; plus targeted summits That subtle distinction opened the door to a brand-new assay format. For GPCRs, fluorescent ligands have quietly become one of the most versatile technologies—supporting Subtype specificity:  selectively track receptor subtypes in complex brain tissue.

This makes it an ideal candidate for GPCR research, where accuracy in detecting subtle signaling changes

blood-brain-barrier (BBB) and the complexity of the central nervous system (CNS) pose a challenge for developing successful central role in neuronal signaling and have been used to treat these diseases with varying degrees of success One of the biggest hurdles is the understanding and correct targeting of the different receptor subtypes promotes nucleotide release from, and activation of, the G protein α-subunit. Greater specificity : allows for selective tracking of receptor subtypes in complex brain tissues.

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Ignore these forces, and your “selective” agonist may deliver surprises the first time it meets a patient Surface vs. This section raises a critical design question for teams Are you sure your “antagonist” is enough—or Subscribe today and get direct access to decades of pharmacology experience that turn complex systems Subscribe to The Kenakin Brief today ➤

GPCR Reagent Portfolio pHSense™ is the latest addition to Revvity’s GPCR reagent portfolio , which supports Its GPCR research tools  support discovery teams and academic labs with precision reagents and validated