The aim of this study was to quantify enzymes and transporters in 20 human kidney cortex fractions. Using targeted accurate mass retention time (AMRT) and global proteomic approaches, 6 UGTs, 3 CYPs, 22 transporters, 1 adhesion and 1 plasma membrane marker were quantified; Eight of these proteins were identified for the first time in the kidney. The global proteomic method identified >4000 proteins. Kidney CYP2B6, CYP3A5 and CYP4F2 showed generally low expression.