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Drug discovery often assumes receptor inhibition follows simple rules—agonist binds, antagonist blocks That paper quantified how one drug could block another’s access to a receptor—a framework that Heinz The Quick Glance: pA₂ as Shortcut Sometimes, discovery projects don’t have the luxury of full curve analyses Built for pharmacologists refining tools, discovery teams solving bottlenecks, and leaders seeking credible

A bitter anti-inflammatory drug binds at two distinct sites of a human bitter taste GPCR Lior Peri ,   discovery GPCR Classes Pathios Therapeutics Announces Dosing of First Patient in Phase 1/2 Clinical Discovery February 15 - 19, 2025 | BPS 2025 February 16 - 21, 2025 | Harnessing the Power of Advanced Multimodal Approaches to GPCR Drug Discovery March 12 - 14, 2025 | NextGen Biomed 2025 March 25 - 28 Discovery Chemistry April 24 - 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR

foundational lesson, Terry Kenakin dives deep into a widely used, often misunderstood tool in early drug discovery: the calcium assay. transient—giving rise to a “hemi-equilibrium” window that can significantly distort your understanding of drug

GPCR Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled targets, remain central in modern targeted drug discovery. The 19th Annual GPCR-Based Drug Discovery conference (October 2-3, 2024, in Boston and online) gathers Join us October 2-3 at the GPCR Drug Discovery Conference . discovery September 30 - October 3, 2024 | 22nd Discovery on Target October 2024 | Biologics US 2024

protease activated receptor 4 (PAR4) in mouse models of acute and chronic kidney injury GPCR Binders, Drugs Sosei Heptares to take back GPCR agonist after GSK changes course All-rounder among receptors inspires drug Exhibition February 11 - 14, 2023 | 2024 BPS Annual Meeting March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29 , 2024 | Ligand Recognition and Molecular Gating Conference April 1 - 4, 2024 | 19th Annual Drug Discovery

GPCR Partnered Events March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit Exciting news! We're partnering again with the 3rd GPCRs - Targeted Drug Discovery Summit in Boston on March 5-7, 2024 Discovery with STAGS Machine Learning Model Three GPCR Companies Earn Prestigious Best Places to Work discovery Aelis Farma Achieves Milestone: Randomisation Concludes in Largest-Ever Phase 2b Clinical Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual

description of the company was very intriguing: a biology focused, small molecule focused, smaller drug discovery company with a great work environment.  biochemical, cell based, and radioligand binding assays to enable SAR, MOA, lead optimization, and new target discovery Top candidates will have a solid foundation in GPCR pharmacology as well as some experience in drug discovery

November 25 - 27, 2024 | 1st Virtual GPCR Forum Conference November 26 - 28, 2024 | GPCRs-Targeted Drug Discovery Summit Europe July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology Sapap3 knockout mice Orphan GPCRs in Neurodegenerative Disorders: Integrating Structural Biology and Drug Discovery Approaches Altered PLCβ/IP3/Ca2+ Signaling Pathway Activated by GPRCs in Olfactory Neuronal

In drug discovery, intuition creeps in. Eyes deceive. The first trap in drug discovery is relying on visual inspection. Scatter can masquerade as signal. Statistical Methods in Drug Discovery: Your Edge If you’re still making calls by sight, habit, or tradition It’s a shift in how you approach discovery. And once you make that shift, you’ll never go back. Here, you’ll find: Weekly lectures  that sharpen the tools you actually use in discovery A growing on-demand

The potentially low pH at tissue targeted by opioid drugs in pain management could impact drug binding to the opioid receptor, because opioid drugs typically have a protonated amino group that contributes

We're zooming back to the future of GPCR discoveries. Discovery and Antibody Innovation: DeciBio Q&A with Sean McClain, Founder & CEO, and Zach Jonasson, Discovery February 15 - 19, 2025 | BPS 2025 February 16 - 21, 2025 | Harnessing the Power of Advanced Multimodal Approaches to GPCR Drug Discovery March 12 - 14, 2025 | NextGen Biomed 2025 March 25 - 28 Discovery Chemistry April 24 - 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR

GPCR University Course, ‘Applying Pharmacology to Drug Discovery,’ led by Dr. cardiomyocyte death after myocardial infarction through β1 adrenergic receptor GPCRs in Neuroscience Discovery discovery in endocrinology and metabolism Reviews, GPCRs, and more Butyrate as a promising therapeutic target in cancer: From pathogenesis to clinic (Review) Will the hype of automated drug discovery finally Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual

Kenakin and Hoare on '   Applying Pharmacology to Drug Discovery ' and ' Advanced Data Analysis for GPCR Determining mechanisms of action for new GPCR ligands Key elements of a comprehensive and effective GPCR discovery cAMP Olanzapine manipulates neuroactive signals and may onset metabolic disturbances GPCR Binders, Drugs GPCRs and mRNA antigens enable drug discovery and development Mapping GPCR-RAMP complexes with MolBoolean discovery October 2024 | Biologics US 2024   October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry

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

📰 GPCR Weekly News, July 22 to 28, 2024 In the fast-paced world of pharmaceuticals and drug discovery , efficacy, co-operativity) Mechanisms of action for new GPCR ligands Essentials for effective GPCR discovery discovery, a biophysics perspective Bio-Rad Adds Rapid Bispecific Antibody Prototyping and Screening Services to Pioneer Antibody Discovery Platform GPCR Events, Meetings, and Webinars November 5 - 7, discovery October 2024 | Biologics US 2024 October 2 - 4, 2024 | 9th GPCRs in Medicinal Chemistry October

GPCR University course, 'Applying Pharmacology to Drug Discovery,' led by Dr. GPCR Partnered Events March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit Join us at the 3rd Discovery March 13 - 15 | 9th German Pharm-Tox Summit March 23 - 24, 2024 | Ligand Recognition and Molecular 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 1 - 4, 2024 | 19th Annual Drug Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual

Discovery, led by Dr. GPCR Partnered Events March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit Join us at the 3rd Discovery March 13 - 15 | 9th German Pharm-Tox Summit March 23 - 24, 2024 | Ligand Recognition and Molecular 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 1 - 4, 2024 | 19th Annual Drug Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual

Discovery,' which will be led by Dr. GPCR Partnered Events March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit Join us at the 3rd , and more Insights on discovery, efficacy, safety and clinical applications of ghrelin receptor agonist Discovery March 13 - 15 | 9th German Pharm-Tox Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual

β-arrestin1 is an E3 ubiquitin ligase adaptor for substrate linear polyubiquitination GPCR Binders, Drugs Discovery Orion’s VP Drug Discovery, Dr. Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29 , 2024 | Ligand Recognition and Molecular Gating Conference April 1 - 4, 2024 | 19th Annual Drug Discovery Postdoctoral Associate in Computational Chemistry/Biophysics Post-Doctoral Associate Team Leader Antibody Discovery

. _______________ Keyword Cloud: GPCR drug discovery , G protein-coupled receptors , GPCR webinar series

Why Culture Matters in Drug Discovery You can’t innovate under pressure. From Lab Bench to Boardroom His work at Alkermes didn’t just improve drug screening outcomes, it redefined

Drugs like Ozempic will change the world GPCR Events, Meetings, and Webinars November 5 - 7, 2024 | 16th Discovery Summit Europe NEW December 10 - 12, 2024 | Pharmacology 2024 NEW January 13 - 16, 2025 | PepTalk Discovery NEW February 15 - 19, 2025 | BPS 2025 NEW February 16 - 21, 2025 | Harnessing the Power of Advanced Multimodal Approaches to GPCR Drug Discovery NEW March 12 - 14, 2025 | NextGen Biomed 2025 Discovery Chemistry NEW   April 24 - 27, 2025 | American Physiology Summit 2025 NEW April 25 - 30, 2025

GPCR University course, Applying Pharmacology to Drug Discovery, led by Dr. GPCR Partnered Events March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit  We're partnering again with the 3rd GPCRs - Targeted Drug Discovery Summit in Boston on March 5-7, 2024. 24 - 29, 2024 | Ligand Recognition and Molecular Gating Conference April 1 - 4, 2024 | 19th Annual Drug Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual

This concept is gaining significant attention in drug discovery, especially in the context of G protein-coupled The concept of biased agonism has been effectively leveraged in drug discovery, as demonstrated by the Tirzepatide's success underscores the potential of designing drugs that selectively target beneficial Christopoulos, Signalling bias in new drug discovery: detection, quantification and therapeutic impact Nat Rev Drug Discov, 2013. 12 (3): p. 205-16. 2.         

Portfolio with Granted Patents in Australia and Singapore Crinetics Announces FDA Acceptance of New Drug Discovery February 15 - 19, 2025 | BPS 2025 February 16 - 21, 2025 | Harnessing the Power of Advanced Multimodal Approaches to GPCR Drug Discovery March 12 - 14, 2025 | NextGen Biomed 2025 March 25 - 28 Discovery Chemistry April 24 - 27, 2025 | American Physiology Summit 2025 April 25 - 30, 2025 | AACR rat pituitary Synthetic GPCRs for programmable sensing and control of cell behaviour GPCR Binders, Drugs

Don’t miss out on insightful resources like '   Applying Pharmacology to Drug Discovery ' and ' Advanced 24, 2024 (four sessions) Topics:  Measuring pharmacologic activity, mechanisms of action, and GPCR discovery agonist-producing Bacillus velezensis ADS024 is efficacious in multiple neuroinflammatory disease models Discovery Discovery GPCR Events, Meetings, and Webinars September 5 - 6, 2024 | 4th Transatlantic ECI GPCR Symposium September 18, 2024 | FREE Webinar - The value of GPCR cell-based assays in drug discovery October 2024

Discovery,’ expertly led by Dr. GPCR Partnered Events March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit. Join Dr. disorders Discovery of a Photoaffinity Probe that Captures the Active Conformation of the Cannabinoid Discovery NEW March 13 - 15 | Biologics 2024 March 13 - 15 | 9th German Pharm-Tox Summit March 23 - Discovery Chemistry April 4 - 7, 2024 | American Physiology Summit April 5 - 10, 2024 | AACR Annual

discovery. discovery. because they are less tractable to standard drug discovery approaches. discovery. of certain groups within the GPCR superfamily to standard drug discovery approaches.

, and more Discovery of (S)-3-(4-(benzyloxy)phenyl)-2-(2-phenoxyacetamido)propanoic acid derivatives Methods & Updates in GPCR Research An image-based abplex method for high-throughput gpcrs antibody discovery Reviews, GPCRs, and more Current strategic trends in drug discovery: the present as prologue Industry Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29 Discovery Chemistry April 5 - 10, 2024 | AACR Annual Meeting NEW April 22 - 23, 2024 | Endocrine Metabolic

contributor article Extracellular signal-regulated kinases – a potential pathway for GPCR-targeted drug discovery Nicola J Smith, Lauren T May, and Natasha L Grimsey for their work on Highlights and hot topics Discovery Engine at ENDO 2024 The Promise of Oxytocin: Novel Approaches for Targeting Oxytocin Receptors June 4, 2024 | Live Webinar ‘It All Starts With a Protein – Protein Sciences as a Key to Success in Drug Discovery’ June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein Mediated Signaling Networks June 25