Acanthopanax senticosus belongs to Araliaceae family and is traditionally used as a tonic. The roots and stems are mainly used as a treatment for hypodynamia, rheumatism, and hypertension, but their frequent use may lead to its extinction. However, comprehensive and simultaneous analysis of the remaining parts were still limited, and needs to reorganize for standardization of functional foods. In this study, 50 phenolic compounds and 82 triterpenoid saponins from the shoots, leaves, fruits, and stems of A. senticosus were characterized using UPLC-QTOF-MS and UPLC-QTRAP-MS/MS. Among them, 57 new compounds were detected as the cis and malonyl-bound phenolic acids and were structural isomers of Acanthopanax flavonoids and saponins. All compounds were absolutely/relatively quantified, and shoots had the highest content. Antioxidant and α-glucosidase inhibitory activity were performed, followed by evaluation of structure-activity relationships. Both activities of all tested extracts and saponins showed remarkable efficacy and affected by the C-23 hydroxylation, the C-20(29) double bond, and the presence of rhamnose. These detailed profiling can be used as fundamental data for increasing the utilization of A. senticosus and developing them into functional foods.