In the current investigation, research on OAT1 structures reveals key insights into kidney drug transport mechanisms(1). OAT1 is located in kidney and control the uptake and excretion of various organic anions, drugs, and toxins . Inhibiting OAT1 will decrease the drug excretion and hence increases the drug concentration in blood. To designing inhibitors against this receptor a deeper understanding of OAT1 drug binding site is crucial. We hypotheses that that the ligands bind at the center of the drug transport channel of the transorter protein.