In the current study, we demonstrate that Compound 1 exhibits key pharmacological properties that are pre-requisite to its potential suitability as a scaffold for PAM drug development, including low intrinsic activity, selectivity, maintenance of activity across CCK1R from species relevant to preclinical obesity drugs, augmentation of the predominant circulating form of CCK, and activity in disease-mimicking conditions. Here, CCKAR is linked to Obesity.