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Hit identification and structural optimization. (A) Flowchart for the screening process of hit compound (Hit-1). (B) Structural optimization of Hit-1 led to the identification of a potent GPR34 antagonist YL-365. Bioactivities of compounds were measured by the Tango assay. Dose–response curves of Hit-1 and YL-365 are shown. IC50 values are mean ± SD from three independent experiments.
