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Rice (Oryza sativa) is an excellent resource; it comprises 25% of the total caloric intake of the world's population, and rice plants yield many types of bioactive compounds. To determine the number of metabolites in rice and their chemical diversity, the metabolite composition of cultivated rice has been investigated with analytical techniques such as mass spectrometry (MS) and/or nuclear magnetic resonance spectroscopy and rice metabolite databases have been constructed. This review summarizes current knowledge on metabolites in rice including sugars, amino and organic acids, aromatic compounds, and phytohormones detected by gas chromatography–MS, liquid chromatography–MS, and capillary electrophoresis–MS. The biological properties and the activities of polar and nonpolar metabolites produced by rice plants are also presented. Challenges in the estimation of the structure(s) of unknown …