In this study, Methanolic extracts of Euphorbia denticulata parts (flowers, leaf, stem, and mix of aerial parts) were assessed for a panoply of bioactivities. Inhibitory potential against key enzymes involved in diabetes (α-glucosidase and α-amylase), obesity (pancreatic lipase), neurodegenerative diseases (cholinesterases), and hyperpigmentation (tyrosinase) was evaluated. The antioxidant and antibacterial properties were also assessed. The total phenolic, flavonoid, and phytochemical profile were established using HPLC/DAD and molecular modelling studies on specific target compounds were performed in silico. The flower extract was found to be rich in phenolics and flavonoids, (60.11 ± 1.40 mgGAE/g and 42.04 ± 0.16 mgRE/g respectively), which tend to correlate with the high radical scavenging activity of this extract (120.34 ± 3.33 mgTE/g and 165.42 ± 2.16 mgTE/g for DPPH and ABTS respectively). Catechin, epicatechin, gallic acid, p-OH-Benzoic acid, rosmarinic acid, and epigallocatechin gallate, found in significant abundance in the extracts were assessed using molecular modelling with the aim to study their docking properties on a set of six enzymes used in this study. The extracts were moderately effective with MIC values ranging between 1.56 to 6.25 mg/ml, but potent growth inhibitors of MRSA strains. Results amassed herein can be used as a stimulus for further studies geared towards the development of novel phyto-pharmaceuticals.