Insights That Move the GPCR Field Forward

Discovery programs rarely fail because a molecule “did nothing.” They fail because a molecule behaved exactly as the underlying system allowed—amplified, buffered, redirected, or reshaped by layers of receptor biology that weren’t accounted for. The October 30th AMA with Dr. Kenakin highlighted a fundamental truth: GPCR systems do not offer stable, proportional input–output relationships. Receptor density, constitutive activity, coupling efficiency, local signaling archit