Insights That Move the GPCR Field Forward

Drug discovery often assumes receptor inhibition follows simple rules—agonist binds, antagonist blocks, and data fit neatly into predictable curves. Yet, any pharmacologist who’s pushed beyond textbook theory knows: biology rarely plays fair. Schild analysis remains one of the few conceptual anchors that can tell us when “simple” truly is simple—and when deeper receptor dynamics are at play.

Don’t let curve shapes deceive you. In this blog, Dr. Terry Kenakin unpacks why dose-response shifts aren’t definitive proof of antagonist mechanism. Learn how binding kinetics—not just appearance—distinguish competitive from non-competitive antagonism, and why assumptions can mislead drug discovery decisions. If your team relies on DR curves to evaluate receptor blockade, this read will sharpen your approach and help you avoid common pitfalls in mechanism interpretation.