Investigating the phytochemical composition and the biological activities of stems, seeds, and peels of grape, Vitis vinifera was achieved. HPLC/DAD analysis of the three crude extracts resulted in the identification and quantification of 21 phenolic acids and 16 flavonoids against authentic compounds. Principal component analysis (PCA) plots were performed to illustrate the variances among the three samples. The quantitative analysis revealed that stem extract contained the highest total phenolic (TP) and total flavonoid (TF) contents and exerted the highest antioxidant effect. Seed extract showed outstanding bactericidal and fungicidal effects against the tested microorganisms. It also demonstrated the highest cytotoxic action against human cancer cell lines MCF-7 and HCT-116, while peel extract was the most active against PC-3 and HEPG2. PCA allowed the discrimination between grape samples; peels could be positively associated with apigenin. Pearson's correlation analysis was carried out between TF and TP contents of the tested extracts and their biological activities. Correlation coefficient (r) showed a significant, strong positive correlation between DPPH scavenging power and TP, TF contents, while the cytotoxicity and antimicrobial activities were medium positive to negatively correlated to TP and TF contents. Moreover, biosafety studies for the extracts were carried out and proved the safety of all extracts, whereas LD50 was more than 5 g/kg b. wt. Additionally, serum biomarkers, body and organs weights did not show any deviation from the normal rat's scale. Genotoxicity and antimutagenicity assays proved that the examined grape extracts had the potential to reverse the genotoxicity of cyclophosphamide, an anticancer medication.