The expression and transport functions of organic anion transporters are modified in liver diseases, and therefore the vascular clearances of endogenous and exogenous organic anions that are taken up by these transporters have been used to assess liver diseases in patients. More recently, liver imaging with hepatobiliary contrast agents, tracers, and dyes that cross hepatocytes through the organic anion transporting polypeptides (OATPs)-multidrug resistance-associated proteins (MRPs) pathway were developed to detect and characterize focal lesions and to assess the severity of diffuse liver diseases. This review focuses mainly on magnetic resonance imaging and highlights the growing interest in imaging the OATPs-MRP2 pathway to better understand liver diseases. Imaging provides noninvasive measurements of tissue concentrations that result from the interplay between influx and efflux membrane transport systems in normal or injured hepatocytes. Imaging with magnetic resonance hepatobiliary contrast agents improves the detection and the characterization of hepatic focal lesions. New developments of imaging to assess liver function and understand the hepatocellular concentrations of contrast agents are discussed.