Validation of Y4R PAM activity and subtype selectivity of initial Ca2+-flux-based screen hit compounds in an inositol phosphate accumulation assay.

(A) Compound structures. (B) Effect of 10 μM compound on submaximal YR activation by 1 nM ligand, which represents EC20-EC60 (Y1,2,5R: NPY; Y4R: PP). Data represent the mean ± SEM of two independent experiments each performed in quadruplicate (*** p ≤ .001 Bonferroni).