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April 2022 Design Pharmaceuticals Closes $5 Million Pre-series A Round to Accelerate Commercialization --Design Pharmaceuticals, a company redesigning small molecule drug discovery, today announced the closing Design Pharmaceuticals’ platform is based on ultrahigh-throughput technologies that biomine drug-like

April 2022 "SAN DIEGO, April 12, 2022 — Crinetics Pharmaceuticals, Inc. (Nasdaq: CRNX), a clinical-stage pharmaceutical company focused on the discovery, development and commercialization

If your team is designing covalent or tight-binding candidates, these principles reduce surprises and Designing for penetration —balance on/off rates to reach inner tissue, not just peripheries. Watch our new trailers for a preview of expert-led GPCR training designed for scientists and drug hunters Jens Carlsson shares how structure-based design, molecular dynamics, and smart collaboration turn models Kenakin… sorely needed in the field." — DrGPCR University Attendee 🚀 Join now — and learn to design

December 2021 Crinetics Pharmaceuticals announced the formation of an independently operated new company and Crinetics to Collaborate on Multiple Additional targets SAN DIEGO, October 18, 2021 — Crinetics Pharmaceuticals (Nasdaq: CRNX), a clinical stage pharmaceutical company focused on the discovery, development, and commercialization

March 2022 Crinetics Pharmaceuticals Expands Executive Team With Appointment Of James Hassard As Chief Commercial Officer "SAN DIEGO – March 1, 2022 – Crinetics Pharmaceuticals, Inc. (Nasdaq: CRNX), a clinical stage pharmaceutical company focused on the discovery, development, and commercialization

Innovative design approach emphasizing scientific principles over speculation. GPCR News delivers a toolkit of practical innovations—from drug design strategies that anticipate physiological Terry's Corner – Designing Drugs That Anticipate Physiological Pushback Most GPCR programs don’t fail week’s Terry’s Corner  exposes the unseen physiological “opponents” your molecule faces—and how to design Design smarter inotropes:  Dobutamine’s α-activity harnesses baroreflexes to increase contractility without

In recent years, pharmaceutical companies have begun to utilize cryo-EM for structure-based drug design In this review, we discuss recent instructive examples of impacts from cryo-EM in therapeutics design

If you’ve ever trusted a Ki value without asking how  it was measured, you’ve already stepped into the trap. In drug discovery, equilibrium constants look tidy. But biology isn’t tidy. Onset and offset rates (not just “final numbers”) decide which drugs succeed in patients and which ones die in development. Affinity snapshots alone won’t save your pipeline. Kinetics will. This session gives you precisely that. By the end, you’ll know how to confirm true equilibria, detect hidden drug activities, and separate safe candidates from toxic ones long before clinic. No more blind spots, only decisions rooted in reality. In this session, you'll gain: ✅ Tools to confirm true equilibrium and avoid potency errors from premature reads ✅ Methods to detect hidden mechanisms—mixtures, dual effects, or time-dependent inhibition—through curve shapes and kinetics ✅ A framework to classify antagonists and rank compounds by offset rate, using rapid calcium assays Potency Is a Ratio of Rates Two ligands compete for the same receptor. Which wins? Not just the one with higher affinity, but the one that gets there faster and leaves slower. Think of it like catching a train: two passengers have tickets (affinity), but only the one who sprints to the platform on time (fast onset) and stays seated (slow offset) actually gets the ride. Ignore this, and you’ll misrank compounds. Respect it, and you’ll see why drugs with identical Ki values diverge in vivo. This is the first trap: assuming equilibrium when you haven’t reached it.  Curves that “look fine” may hide non-equilibrated systems. The fix? Use curve shapes as diagnostics: flattened, biphasic, or lagging responses aren’t noise. They’re telling you to wait. When Equilibrium Lies Sometimes, numbers don’t add up. You calculate an equilibrium value that requires a physically impossible onset rate. That’s your signal: kinetics are moving faster than your tools can measure. It’s like calculating a runner’s pace and realizing they’d have to break the sound barrier to make the numbers work. The math itself is your clue that something else is happening. This is the second trap: trusting impossible math. If you ignore it, you risk false certainty. If you detect it, you gain texture that equilibrium constants alone can’t provide. And this texture matters; kinetics have separated safe dopamine antagonists from those with extrapyramidal side effects. Hidden Mixtures, Hidden Risks Peptides degrade. Drugs carry dual mechanisms. At equilibrium, these effects cancel. But kinetics unmasks them. Instead of clean monophasic curves, you’ll see biphasic signatures or sequential shifts—first cholinesterase inhibition, then receptor blockade. This is the third trap: assuming one mechanism when two are in play. Catch it early, and you avoid wasting months chasing the wrong SAR. The Hemi-Equilibrium Problem Calcium assays look simple. But if your antagonist has a slow offset, you’ll see depressed maximal responses that equilibrium theory can’t explain. This is the fourth trap: classifying antagonists as weak when they’re just slow. Flip it around, and you’ve got a shortcut: use depression of max in calcium assays to rapidly rank offset rates, and predict in vivo coverage before you ever dose an animal. Fractal Potency: The Illusion of Nothing, Then Everything Measure too soon, and low concentrations look inert. Suddenly, at higher doses, you see an exaggerated ‘bang’ of effect. It’s like waiting for popcorn: at first, nothing happens, then suddenly the bag explodes with pops. But that’s timing, not a different kind of corn. That’s not pharmacology. That’s kinetics. This is the fifth trap: misclassifying your antagonist because you didn’t wait. The cure is simple: extend equilibration. Once you do, the irregular potency vanishes, and the true profile emerges. What You’ll Walk Away With By the end of this session, you won’t just “know about kinetics.” You’ll know how to use  kinetics to sharpen decisions: Confirm whether your system has truly equilibrated Detect hidden activities before they waste resources Classify antagonists by offset rate without waiting on PK data Spot time-dependent inhibition that signals toxic liabilities Avoid being fooled by fractal potency artifacts This isn’t academic nuance. It’s the difference between building a solid pipeline and chasing ghosts. Kinetics in Drug Discovery: Your Edge If you’re still treating potency as a static number, you’re missing half the story. Kinetics turns confusion into clarity, reveals risks earlier, and helps you rank compounds by the criteria that matter most in patients. This isn’t just another lecture. It’s a shift in how expert drug hunters see pharmacology. And once you see it, you’ll never go back. Unlock “Kinetics: Advanced Applications” Only in Terry’s Corner Why Terry’s Corner Most pharmacology training stops at equilibrium values. But discovery doesn’t. The reality is dynamic—ligands arrive, depart, and interact in ways that standard assays often miss. That’s where Terry’s Corner changes the game. Here, you’ll find: Weekly lectures  that sharpen the tools you actually use in discovery A growing on-demand library  of lessons you can revisit whenever you need them Exclusive access  to the next AMA session Direct engagement opportunities  through AMAs and topic suggestions Practical insights  distilled from decades of pharmacology experience Whether you’re validating assays, refining kinetic models, or deciding which leads to advance, Terry’s Corner gives you the frameworks to detect hidden liabilities and uncover real drug potential. See beyond the equilibrium. Make decisions with confidence. 🟢 40 years of expertise at your fingertips: Explore the complete library ➤ ✳️ Want to know what’s inside? Read the latest articles ➤ Stay sharp between lectures. Subscribe to The Kenakin Brief  today ➤

Rational Drug Design One immediate application of this research lies in rational drug design . By identifying key β2AR residues that influence efficacy and potency, pharmaceutical researchers can This distinction is essential for designing drugs that selectively target these residues to achieve desired For example, orthosteric drug design —in which drugs bind to the receptor’s primary active site—can now Evolutionary Insights and Drug Design From an evolutionary standpoint, the study reveals that residues

July 2022 "Not even a PIPE financing could save X4 Pharmaceuticals from enacting layoffs and trimming

November 2021 Addex's strategic partner The Janssen Pharmaceutical Companies of Johnson & Johnson, Inc Switzerland, November 15, 2021 – Addex Therapeutics (SIX: ADXN and Nasdaq: ADXN), a clinical-stage pharmaceutical pioneering allosteric modulation-based drug discovery and development, today announced that Janssen Pharmaceuticals , Inc., part of the Janssen Pharmaceutical Companies of Johnson & Johnson, has successfully completed

June 2022 "CRN04894 Selected for Oral Presentation SAN DIEGO, June 8, 2022 — Crinetics Pharmaceuticals

So I designed my own PhD program,” Sokhom shared. navigating work, life, and scientific ambition, Sokhom Pin proves it’s possible to have it all, if you design

Supporting them is a medicinal chemist who can design and synthesize new scaffolds when commercial libraries The power of this design lies not in its independence but in its interdependence . And experiments are better designed because expectations are realistic. The most effective discovery programs are structured like Carlsson’s: modeling designed with downstream And he prioritizes shared purpose , designing each project with the next experiment in mind.

. ✅ Practical strategies  for using receptor trafficking data and system set-points to design cleaner Every ligand you design enters a system that is already balancing opposing forces—vasoconstriction vs Reflexes as Drug Design Partners Not all reflexes are enemies. Some can make a mediocre drug shine. The teaser question How could you design your next lead to recruit the body’s own feedback loops in your This section raises a critical design question for teams Are you sure your “antagonist” is enough—or

When he returned to Sweden for his PhD, he focused on small molecule design. behavior post hoc, his group began developing workflows and strategies that could drive experimental design

Innovative Approaches in GPCR Drug Discovery: Designing Precise Solutions for GPCR Challenges. That’s exactly what Terry’s Corner delivers this week: a deep dive into molecular creativity, rational design compounds. • The Power of Structure : How privileged scaffolds and rational design open the door to dual activity and precision. • Cheminformatics to Biologics : GPCR-focused chemical design is evolving—fast Whether you’re designing the next assay, scouting a new therapeutic angle, or exploring career pivots

insights not just to explain receptor–ligand interactions after the fact, but to forecast outcomes and design When existing compounds are exhausted, bespoke ligands are designed and synthesized in-house. Can we design compounds that trigger biased signaling? But part of their rigor lies in restraint. GPCR Premium Ecosystem  for advanced insights into structure-based modeling, ligand design, and experimental

October 2022 GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches This approach can expand the repertoire of adenosine receptor antagonists that can be designed based

October 2022 Design and validation of recombinant protein standards for quantitative Western blot analysis

bioinformatics are powerful tools to build modular, reproducible, and reusable pipelines for computer-aided drug design

differences impeded the use of predicted structure models in the functional study and structure-based drug design

with Domain Therapeutics and Université de Montréal for GPCR-Targeted Drug Discovery "Apr.19.2022 Ono Pharmaceutical

It’s a design space , not a binary choice, and penetration is just the beginning. Designing Strategically with Irreversible Drug Binding in Mind When irreversible mechanisms are designed featuring real questions from discovery scientists tackling enzyme kinetics, receptor bias, and assay design Join Terry’s Corner and get: Frameworks proven in real discovery programs On-demand lessons  designed Weekly lectures  that sharpen your command of how enzyme activity drives pharmacokinetics and drug design

Trevena Announces Submission of New Drug Application in China for OLINVYK® by its Partner Jiangsu Nhwa Pharmaceutical The NDA was submitted by Trevena’s partner, Jiangsu Nhwa Pharmaceutical, and follows completion by Nhwa

October 2022 "While the role of G-protein-coupled receptors (GPCR) in cancer is acknowledged, their underlying signaling pathways are understudied. Protease-activated receptors (PAR), a subgroup of GPCRs, form a family of four members (PAR1-4) centrally involved in epithelial malignancies. PAR4 emerges as a potent oncogene, capable of inducing tumor generation. Here, we demonstrate identification of a pleckstrin-homology (PH)-binding motif within PAR4, critical for colon cancer growth. In addition to PH-Akt/PKB association, other PH-containing signal proteins such as Gab1 and Sos1 also associate with PAR4. Point mutations are in the C-tail of PAR4 PH-binding domain; F347 L and D349A, but not E346A, abrogate these associations. Pc(4-4), a lead backbone cyclic peptide, was selected out of a mini-library, directed toward PAR2&4 PH-binding motifs. It effectively attenuates PAR2&4-Akt/PKB associations; PAR4 instigated Matrigel invasion and migration in vitro and tumor development in vivo. EGFR/erbB is among the most prominent cancer targets. AYPGKF peptide ligand activation of PAR4 induces EGF receptor (EGFR) Tyr-phosphorylation, effectively inhibited by Pc(4-4). The presence of PAR2 and PAR4 in biopsies of aggressive breast and colon cancer tissue specimens is demonstrated. We propose that Pc(4-4) may serve as a powerful drug not only toward PAR-expressing tumors but also for treating EGFR/erbB-expressing tumors in cases of resistance to traditional therapies. Overall, our studies are expected to allocate new targets for cancer therapy. Pc(4-4) may become a promising candidate for future therapeutic cancer treatment." Read more at the source #DrGPCR #GPCR #IndustryNews

One such platform is the chemogenetic DREADD (designer receptor exclusively activated by designer drugs

A conserved intracellular allosteric binding site (IABS) has recently been identified at several G protein-coupled receptors (GPCRs). Starting from vercirnon, an intracellular C-C chemokine receptor type 9 (CCR9) antagonist and previous phase III clinical candidate for the treatment of Crohn's disease, we developed a chemical biology toolbox targeting the IABS of CCR9. We first synthesized a fluorescent ligand enabling equilibrium and kinetic binding studies via NanoBRET as well as fluorescence microscopy. Applying this molecular tool in a membrane-based setup and in living cells, we discovered a 4-aminopyrimidine analogue as a new intracellular CCR9 antagonist with improved affinity. To chemically induce CCR9 degradation, we then developed the first PROTAC targeting the IABS of GPCRs. In a proof-of-principle study, we succeeded in showing that our CCR9-PROTAC is able to reduce CCR9 levels, thereby offering an unprecedented approach to modulate GPCR activity. Read full article

This research topic is designed to stimulate discussion and fuel the scientific direction of future GPCR lectures, classified industry news, priority event alerts, job opportunities, and insider commentary—designed

, an international biopharmaceutical company and world-leader in GPCR1-focused structure-based drug design