Why Kinetics Matter More Than Kd in GPCR Drug Discovery
- Dr. GPCR News
- Jul 24
- 4 min read
Updated: Jul 28
Welcome GPCR Fans,
Every discovery-phase decision you make shapes your entire pipeline trajectory—and understanding when equilibrium affinity falls short is no longer optional.
That’s exactly what Terry’s Corner delivers this week: real-world kinetic frameworks to help you move faster and make smarter choices.
Breakthroughs this week: Structure-based discovery of positive allosteric modulators of the A1 adenosine receptor; GPR171 is necessary for normal physiological functions and mood-related behaviors in males, but not females; Discovery on Target GPCR Drug Discovery.
🔍 This Week in Premium: Sneak Peek
A curated preview of this week’s Premium classified content — designed to keep you ahead without noise or delays:
Industry insights: Structure-Based Drug Design Summit; AI-Powered GPCR Research; Lab-in-the-Loop Hit Discovery advances.
Upcoming events: 5th MMCS New Trends in Drug Discovery; GPCR-UK Network Meeting; neuroGPCR Symposium.
Career opportunities: Principal Scientist - In Vitro Pharmacology; Senior Scientist, Molecular Pharmacology; PhD position in proteomics and GPCR signaling.
Must-read publications: GPCRchimeraDB: Database of engineered GPCR designs.
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Terry’s Corner: Why Binding Kinetics Matter More Than Affinity
In drug discovery today, time wasted is opportunity lost. Yet too many programs rely solely on affinity metrics—Kd—as proxies for in vivo behavior, missing a critical layer of insight: kinetics.
Terry Kenakin’s latest lecture in Terry’s Corner delivers exactly what your discovery teams need now: a pragmatic framework to interpret kinetic binding experiments and recognize when a drug’s rate of onset and offset matter more than affinity itself.
Prevent wasted cycles: Avoid costly delays caused by false positives from static affinity readouts.
Gain operational clarity: Learn how kinetics signal which compounds will truly perform in vivo—under competitive, real-world conditions.
Stay ahead of competitors: Know when your data reflects equilibrium and when to probe deeper, ensuring your team doesn’t misinterpret key signals.
Premium Members get 50%+ discount when they join Terry’s Corner.
🔒 Available only in Terry’s Corner - Premium Members get an exclusive discount
🗣️ “Dr. Kenakin is a masterful teacher and communicator—and a leading expert in our field.” — Dr. GPCR University Course Attendee
Dr. GPCR Podcast : From Personal Pain to Scientific Purpose: Alex Serafini’s Journey
We sit down with Dr. Alex Serafini, whose unconventional path—from patient to scientist—exemplifies why personal mission matters in translational research.
Serafini’s early struggles with chronic pain sparked a career focused on innovating where pain management has long stagnated. His work challenges outdated targets, explores overlooked roles of GPCRs and RGS proteins in pain, and seeks to redefine translational models for patient realities.
Redefine your playbook: Why Serafini believes that pain research needs to start from clinical phenotype and work backward.
Explore blind spots: The underestimated role of GPCRs and RGS proteins in chronic pain mechanisms.
Rethink translational success: How post-COVID insights and unconventional decision-making shaped Serafini’s high-impact projects.
Event: Where the Next Decade of GPCR Therapies Will Be Defined
The 20th annual Discovery on Target GPCR-Based Drug Discovery meeting is where the next wave of therapies—from allosteric modulators to computational targeting—will take shape.
If you’re not there, you’re missing an opportunity to benchmark your strategy against the best in the field. Terry Kenakin’s featured talk on “The Kinetics of Allostery” offers a rare live glimpse into advanced kinetic thinking—but for full, actionable frameworks, only Terry’s Corner members get exclusive on-demand access.
Benchmark your roadmap: See where competitors are heading before they act.
Identify emerging targets: Allosteric modulators, biased ligands, and kinetic frameworks will dominate the next wave.
Get exclusive discounts: Secure your seat now with code DRGPCR25 for $200 off.
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#GPCR #DrGPCR #BindingAffinity #Pharmacology #DrugDiscovery #LeadOptimization #TerryKenakin #EmergingDrugHunter #EfficientDiscovery #PipelineAcceleration
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