Search Results

Onset and offset rates (not just “final numbers”) decide which drugs succeed in patients and which ones 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. them Exclusive access  to the next AMA session Direct engagement opportunities  through AMAs and topic suggestions Subscribe to The Kenakin Brief  today ➤

Upcoming events:  “Drug Discovery at Superluminal Speeds”; and Discovery on Target 2025—GPCR track you Engineer assays on purpose:  Set ranges, controls, and system sensitivity to surface mechanism—before Also super-valuable for those of us learning how to teach pharmacology." — DrGPCR University Attendee

Flow cytometry, a laser-based method, is used to examine single cells suspended in a fluid. Autofluorescence and multiplexing: Using far-red or near-infrared fluorophores can reduce background and support At Celtarys, we support this transition by offering optimized fluorescent ligands specifically designed CELT-240 in flow cytometry binding assays is suitable to measure the affinity of compounds for the D2

Suddenly, your snapshot becomes a forecast . The question was: could crude gp120 supernatant be used instead, without corrupting results? Chemists suddenly have meaningful levers to pull. The lesson: models don’t just need data. Subscriber-driven topics,  so the next lesson addresses your bottleneck. Subscribe to The Kenakin Brief today ➤

Superluminal Medicines: AI/ML Meets GPCR Pharmacology As Ajay continued to explore how GPCR signaling To address this, he co-founded Superluminal Medicines , a biotech company focused on integrating machine Superluminal is building systems that learn from receptor movement, conformational shifts, and complex In August 2025, Superluminal Medicines announced a collaboration with Eli Lilly and Company to advance Takeaway: Ajay Yekkirala’s story is not just about GPCR science or startup success.

insights for drug discovery Hi GPCR Friends, Every week, critical decisions in GPCR research hinge on subtle underpowered studies, this module hands you a practical framework to validate differences, confirm subtle Eliminate subjective calls:  From t-tests to ANOVA and F-tests, know which tool to apply when, so debates This is where the real conversations begin—made possible with the support of NIS, Proteos, and Axxam  

SNAP-tag has been successfully used while preserving activity. It can even study the GPCR distribution within endocytic vesicles and across subcellular compartments Cell-surface protein-protein interaction analysis with time-resolved FRET and snap-tag technologies:

Our Sponsors This event would not be possible without the generous support of our sponsors: NIS Proteos Axxam Axxam is a leading provider of integrated discovery services, supporting the entire drug discovery This comprehensive approach enables Axxam to support clients worldwide in identifying and optimizing

And when decisions ride on subtle shifts, “looks different” isn’t good enough. Subtle shifts vanish in noise. them Exclusive access to the next AMA session Direct engagement opportunities  through AMAs and topic suggestions Subscribe to The Kenakin Brief today ➤ #ttest #ANOVA #poweranalysis #curvecomparison #ftest #assayvalidation

There, she chose to write a review on genetic variation in susceptibility to alcoholism and opioid addiction—a I was staying up super late. I was excited to work on this, till 2 or 3 a.m.” Her current work examines how these substances, when used alone or together, impair breathing in mice This mindset can lead to a more fulfilling and successful career.

While writing a literature review on opioid and alcohol addiction susceptibility, something shifted. Lessons from Catherine’s Story Catherine’s career challenges the idea that success requires a straight Academic success is less about prestige than about impact. That urgency, more than titles, positions, or prestige, is what sustains a lasting career in science.

Blueprint for survival:  Continuous improvement and operational scaffolding—not more hires—are the real

These results support the use of fluorescence-based screening methods as a reliable alternative to classical

Her findings highlight how fentanyl suppresses inhalation while xylazine prolongs exhalation, creating than medicine can adapt, Catherine’s work shows why overdose research must evolve alongside the drug supply That surge mirrors what’s happening nationally. The insight is simple but urgent: the drug supply evolves faster than medicine.   And the illicit supply is moving faster than clinical medicine can adjust.

When a PAM increases radioligand binding but suppresses functional response, it’s not broken pharmacology—it Suddenly, the agonist works . Terry Kenakin An always-growing library of on-demand pharmacology insights The ability to vote on or suggest Subscribe to The Kenakin Brief today ➤ #AllostericPharmacology #GPCR #BindingVsFunction #ReceptorPharmacology

On the other hand, fluorescent ligands have a superior safety and environmental profile.

Moore, was most definitely a success. Now back in Europe, all she can think about is next year’s date, in Dublin, where she is sure she will

CELT-335 was successfully used in assays to determine the pharmacological properties of Δ9-tetrahydrocannabinol When this happens the proximity between donor and acceptor is sufficient for a transmission of energy

New scaffolds modulating the CBRs in both the orthosteric and allosteric sites have been developed, supported of the series developed by Pfizer, including CP5594, gave rise to a new class of abused psychoactive substances GPCRs are not suitable for antibody use due to steric hindrance and reverse binding, thus, other strategies Among them, we have chosen the SNAP-tag, a suicide enzyme technology. Cell-Surface Protein-Protein Interaction Analysis with Time-Resolved FRET and Snap-Tag Technologies:

the minimal chemical modifications in the original ligand, high sensitivity and their extensive and successful (3H) labeled ligands are usually chemically identical to the original, because tritium will usually substitute and more accessible alternative. -            Quantitative cell binding studies : Radioligands have superior

Introduction Dopamine receptors are G-protein-coupled receptors (GPCRs), which have 5 subtypes -D1-5. The estimated Z’ of the assay is 0.71, which is sufficient for HTS standards. Figure 3.   No substantial differences were found between them and the reporter. Figure 4.     These results indicate that CELT-419 is suitable for live-cell assay with automated microscopy. Evaluation of Fluorophores for Optimal Performance in Localization-Based Super-Resolution Imaging.

O-acylisourea rearranging intramolecularly into the N-acylurea.[ 2]     NHS ester amide coupling  is the most suited This property comes from the wide chemical space this reaction can access – we can substitute one reagent Semiquantitative Study of the EDC/NHS Activation of Acid Terminal Groups at Modified Porous Silicon Surfaces Chapter Three - Bioconjugated Materials in the Development of Subunit Vaccines.

Tackling the GPCR Imprecision Problem: Strategic Planning for Sustainable Progress in Complex Systems demands intentional planning and a systematic approach, ensuring every step forward is strategic and sustainable detail, operational process, and strategic decision aligns to create a seamless, predictable pathway to success operational strategy , emphasizing that precision is a continuous, intentional journey towards predictable success biotechs, VCs, and CROs to implement the framework that ensures every step forward is strategic and sustainable

We're launching with 10 on-demand lessons , each featuring:   A short, focused video A concise written summary Your Exclusive Premium Member Benefit:   As a thank you for your continued support of the Dr.

Surely more hands will move the needle. If you want your program to survive, you need a Blueprint for Precision. Not next quarter.

makes a drug “effective,” arguing that kinetic persistence (not binding affinity) determines real-world success But as Kenakin shows, t½ is a surface metric —a combination of clearance and volume of distribution. that explains results in animal models, informs clinical translation, and helps teams avoid late-stage surprises Subscribe to The Kenakin Brief today ➤ #TargetResidenceTime #DrugBindingKinetics #PKPDdissociation #ReceptorPharmacology

Watch Episode 171 Mentoring in science is more than supervising—it’s about shaping the next generation

Terry’s Corner takes you beyond curve shapes into the kinetic and mechanistic realities that separate surface-level transform your program from a series of disconnected efforts into a predictable, de-risked pathway to success Build predictable success:  Use a repeatable improvement framework to turn operational chaos into precision Solve the problem of information overload by getting a curated summary of the key talks and discussions

Beyond the Curve: Questions This Lesson Helps You Answer This lesson pushes you to go deeper than surface-level Why is competitive antagonism  considered reversible and surmountable, while non-competitive antagonism Each subscription includes: Weekly deep dives from Dr. Why now:  GPCR research is accelerating—and the projects that succeed will be those built on clear, accurate Subscribe to The Kenakin Brief today  ➤   #GPCRantagonism #CompetitiveAntagonists #NonCompetitiveAntagonists

But that model is no longer sufficient. Subscribers gain access to: Weekly lessons by Dr.