The aim of this study was to generate multifunctional bioactive peptides from palm kernel cake (PKC) protein. Extracted PKC protein was hydrolyzed using different proteases Antioxidant activity and degree of hydrolysis (DH) of each hydrolysate were evaluated using DPPH• radical scavenging activity assay and O-phthaldialdehyde spectrophotometric assay, respectively. The results revealed a strong correlation between DH and radical scavenging activity of the hydrolysates, where among these, protein hydrolysates produced by papain after 30 h hydrolysis exhibited the highest DH (91 ± 0.1%) and DPPH• radical scavenging activity (73.5 ± 0.25%) compared to the other protein hydrolysates. The papain generated proteolysate was further fractionated based on hydrophobicity and isoelectric point to separate the peptides using RP – HPLC and IEF methods, respectively. Consequently, nine peptides were identified and their respective antioxidant activities were evaluated. All of the nine peptides showed multifunctional activity. The antioxidant activity as measured by radical scavenging activity and chelating activity assays were found to be in the range of 31-71% and 38-56% while those of ACE inhibitory activity and antibacterial were in the range of 40-100% and 10-78%, respectively.. Fractionation of the most effective proteolysate by reverse phase high performance liquid chromatography indicated a direct association between hydrophobicity and radical scavenging activity. Isoelectric focusing tests also revealed that proteolysates with basic and neutral isoelectric point (pI) have the highest radical scavenging activity.The peptides derived from PKC proteolysate were more potent and distinctive compared to those previously reported from the other protein sources.