The administration of radiolabeled compounds with gamma-emitting radionuclides allows real time pursuit of in vivo behavior of the compounds by external counting of the radioactivity. If the compounds possess a specific localization mechanism to target tissue, the image reflects the specific function of the target. This technique has widely been applied in diagnostic nuclear medicine combined with appropriate radionuclides for clinical use. Two strategies have been developed to design radiolabeled compounds for targeted imaging. One constitutes tethering radiolabeled compounds to carrier molecules that possess specific localization mechanisms to target tissue. Another approach constitutes chemical design of radiolabeled compounds, especially metallic compounds, that possess specific localization characteristics to the target per se. In this manuscript, progress of chemical design of radiolabeled compounds for targeted imaging is briefly reviewed. Emphasis is laid on chemical design of radiolabeled antibodies for targeted imaging.