Pharmaceuticals raise concerns for aquatic species owing to their biological activities. It is estimated that nearly 40% of marketed pharmaceuticals target G protein-coupled receptors (GPCRs). Using an in vitro transforming growth factor-α (TGFα) shedding assay, we previously detected antagonistic activities of GPCR-acting pharmaceuticals against angiotensin (AT1), dopamine (D2), acetylcholine (M1), adrenergic family members (β1), and histamine (H1) receptors at up to μg-antagonist-equivalent quantities/L in wastewater in England and Japan. However, which pharmaceuticals were responsible for biological activities in wastewater remained unclear. Here, we used (1) the consumption of GPCR-acting pharmaceuticals, particularly antagonists, as calculated from prescriptions, (2) their urinary excretion, and (3) their potency measured by the TGFα shedding assay to prioritize them for analysis in wastewater in England and Japan. We calculated predicted activities of 48 GPCR-acting pharmaceuticals in influents in England and Japan and identified which were mainly responsible for antagonistic activities in wastewater against each GPCR. Mixtures of pharmaceuticals tested in this study were confirmed to behave additively. The combination of consumption and potency is useful in prioritizing pharmaceuticals for environmental monitoring and toxicity testing.