The consumption of chia seed (Salvia hispanica L.) has increased in recent years due its high content of omega-3 fatty acids and dietary fiber. This seed also has a high concentration of proteins and essential amino acids, becoming a promising source of bioactive peptides. The objective of this review was to identify the composition and the beneficial effects of chia seeds (S. hispanica L.), their proteins, peptides, and their potential impact on human health. The UniProt database was used to identify the chia proteins and their amino acid sequences. The BIOPEP database was used to analyze the peptides's bioactive potential. A total of 20 proteins were cataloged in chia seed, 12 of those were involved in the regular metabolic processes of the plant cells. However, eight proteins were specifically related to production and storage of plant lipids, thus explaining the high concentration of lipids in chia seeds (around 30%), especially omega-3 fatty acids (around 20%). The analyses of amino acid sequences showed peptides with bioactive potential, including dipeptidyl peptidase-IV inhibitors, angiotensin-converting enzyme inhibitors, and antioxidant capacity. These results correlated with the main health benefits of whole chia seed in humans such as antioxidant capacity, and hypotensive, hypoglycemic, and anticholesterolemic effects. Such relation can be associated with chia protein and peptide compositions and therefore needs further investigation in vitro and in vivo.