Assay Volume Control: Your GPCR Drug Discovery Power Lever

Dr. GPCR News
6 days ago
4 min read

Updated: 4 days ago

Enhance your GPCR research with deeper assay insights for more effective results.

This Week’s GPCR Intelligence:

If you want cleaner decisions, start with the system—then the ligand. This week Terry's Corner unlocks a simple lever that separates signal from storytelling, moving programs forward with fewer surprises.

Breakthroughs this week: C. elegans avoids EGCG via SRXA-7 GPCR; a bidirectional GPCR switch modulates immune signaling; a machine-learning tool predicts GPCR–ligand kinetics; and cryo-EM uncovers a new allosteric site on an orphan GPCR.

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Terry's Corner – Assay Volume Control in GPCR Drug Discovery

This week in Terry’s Corner, you’ll learn how dialing receptor expression/coupling up or down reveals hidden partial agonism, “silent” agonism, inverse agonism, and liabilities that derail translation of your GPCR drug discovery program. This isn’t academic—it’s a pipeline filter for reality-aligned decisions.

See the true pharmacology: Lower sensitivity to uncover partial agonism and compare relative efficacy without confounders.
Catch stealth behaviors early: Boost sensitivity to expose weak agonism in “antagonists” or PAMs—before they bite you in vivo.
Design for translation: Map sensitivity ranges to tissue contexts so your plate data predicts what happens in organisms.

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Coming Next Week on the Dr. GPCR Podcast

Starting next week, new episodes will drop bi-weekly on Wednesday mornings — giving you mid-week insights that connect science and strategy.

We kick off with a question that cuts deep: What if your models could actually predict the future?

In this upcoming episode, Dr. Jens Carlsson (Uppsala University) joins Yamina to explore how computational modeling is evolving from explanation to real prediction — and why that shift could reshape GPCR drug discovery.

Prediction, it turns out, is only powerful if you understand its limits.

🎧 Catch up while you wait:

→ Catch up on the latest episodes

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Inside Revvity’s GPCR Journey: How Decades of Discovery Shaped pHSense

From HTRF to pHSense: The Long Game of GPCR Innovation

Most scientists only see the final kit—the catalog number, the plate-ready reagents. But behind every “new” assay is a decade of design, failure, and rethinking.

In this behind-the-scenes look, Dr. Eric Trinquet traces how a series of bold pivots—from Cisbio’s HTRF platform to IP-One and now pHSense—reshaped how GPCR biology gets measured. It’s not just a story about a probe. It’s about how Revvity turns deep science into tools that endure.

Read the full story➤

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🔹 Why now? GPCR innovation is accelerating. Acting on the right signals today prevents tomorrow’s delays—and puts you ahead when budgets and timelines tighten.

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