Fig. 3.

Identification of GLP1-R PAMs from the functional screen of one triazole library. (A) Bioactivity screen of 3,840 crude reaction products from library N3. cAMP accumulation was measured in CHO-K1 cells expressing human GLP-1R treated by different reaction products (50 µM) in the presence of EC₅₀ of GLP-1(9-36) (1.12 µM). Hits that potentiated or suppressed the cAMP production above 90% (relative to the full response of GLP-1(9-36) or DMSO control) were labeled in red or yellow. (B) Dose–response curves of specific new PAMs measured in CHO-K1 cells expressing human GLP-1R in the presence of EC₂₀ of GLP-1(9-36) (0.6 µM). cAMP accumulation was normalized to the full response of BETP. Data represent means ± SEM of three independent experiments performed in triplicate. (C) The structures of new PAMs with dose–response curve data shown in B.