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foundational lesson from Terry Kenakin’s Pharmacology Vault , we unlock the visual language of pharmacology: dose-response In classic Terry style, the lecture walks you through: What dose-response curves are and why they’re 👉 Discover why dose-response curves are the backbone of all pharmacology. Unlock "Dose-Response Curves" now

activity becomes so dominated by experiments, data nuance, and scientific discourse that the organization loses

Juan Jose Fung, Principal Scientist, at GPCR Therapeutics.

March 2022 Inversago Pharma Announces Dosing of First Participant with Metabolic Syndrome in Phase 1B clinical stage biotech company with a unique portfolio of CB1 inverse agonists, announced today the dosing

Why Misreading Antagonism Delays GPCR Drug Discovery If a dose-response curve shifts to the right, you How do the binding kinetics  of an antagonist influence what we actually observe in a dose-response experiment Consider this: Two dose-response curves, side by side.

March 2022 Confo Therapeutics Doses First Subjects In Phase 1 Clinical Trial Of CFTX-1554 For The Treatment medicines targeting G-protein coupled receptors (GPCRs), today announced that the first subjects have been dosed

However, blind assessments of ligand pose quality and affinity prediction have thus far not provided Median ligand RMSD values for top-scored poses were 1.2 Å and 2.0 Å for self-docking and StateMatch/FunctionMatch

That choice determines whether you risk over- or under-dosing, miss safety windows, or miss therapeutic shifts, signaling outcomes, and efficacy profiles. ✅ Practical Perspective:  Why this knowledge reshapes dose–response is not just cleaner assay design but a sharper decision framework for selecting, prioritizing, and dosing Translational Relevance: From Bench to Clinic Misjudging orthosteric vs allosteric behavior can derail dose Recognizing how your ligand interacts with the receptor lets you predict safety margins, dose–response

discovery teams, this means a shorter exposure can yield longer efficacy windows—opening doors to lower dosing Dose prediction models need kinetic nuance—not just Cmax and AUC. For teams running early-stage programs, recognizing this decoupling early can sharpen dose optimization Dosing regimens aligned with biology, not just exposure.

Where’s your dose justification?   How consistent is your manufacturing?   2️⃣ Dose selection logic: Is there a clear, mechanistic, and empirical rationale for how you plan to dose in trials? future label claims , not just scientific curiosity You design preclinical studies that support your dose

It quantifies the degree of agonist blockade using dose ratios . analysis turns receptor pharmacology into detective work, spotlighting mechanistic fingerprints buried in dose–response Derive dose ratios  from those sections only.

In addition, Structure Therapeutics has completed dosing in a single ascending dose (SAD) Phase 1 study

is designing covalent or tight-binding candidates, these principles reduce surprises and accelerate dose missteps by: Preventing kinetic traps —spot PK/PD decoupling early so washouts and C_max don’t mislead dosing

of max in calcium assays to rapidly rank offset rates, and predict in vivo coverage before you ever dose Suddenly, at higher doses, you see an exaggerated ‘bang’ of effect.

cortisol excretion in the presence of sustained, disease-like ACTH concentrations in multiple-ascending dose

recruitment of the CXCR3+ CD8+ T cell in the bronchoalveolar lavage compartment when administered orally at a dose

Complex in Stress and Anxiety Disorders GPCRs in Oncology and Immunology Exacerbating effects of single-dose by the American College of Clinical Pharmacology Sosei and Cancer Research UK announce first patient dosed

“The day we saw dose-dependent internalization in endogenous GLP1R cells—without microscopy—that was

Such studies revealed that tissue response to a given dose of the hormone or its antagonist depends on

Ultimately this could lead to identification of new non-MOR targets that would allow for lower dose utilization

Orthosteric dose increases drive continuously stronger responses; NAMs and PAMs have structural ceilings complex GPCR systems, this boundary is a strategic advantage: NAMs can only shift an agonist curve so far—dose Ranking Partial Agonists Without Losing Meaning Chemists want a single number.

Let's gather 'round for our weekly dose of GPCR News. Congratulations to our Dr. Sosei Heptares Doses First Subject in Phase I Trial with HTL0048149, a First-in-Class GPR52 Agonist for

The PVT appears to provide stimulus salience encoding in a dose- and NPS-dependent manner.

This has implications for everything from dosing frequency  to resistance barriers  in infectious disease

Apply dose-ratios and Schild regressions to derive Kᴮ or pA₂ values that won’t collapse under scrutiny

Solubility poses significant challenges. of adjustments, a scientist on his team presented a data set that transformed everything: a clean, dose-dependent

“We did a full dose-response and saw antagonism—all in one plate-based assay.

That kind of street-level data shapes everything: dosing strategies that reflect actual potencies in

dynamics of hM3Dq [Ca2+]i signaling, increased cell proliferation, and enhanced matrix production in a CNO dose

Financial Results And Provides Corporate Update Sosei Heptares and Cancer Research UK Announce the Dosing