TABLE 3

Effect of intracellular free drug concentration on SLC13A5 inhibition for PF-06649298

CellsNominal IC50Intracellular Free IC50a
μMμM
Human SLC13A5 HEK2930.4118.3
Human hepatocytes1617.5
Fold difference in IC5039∼1
  • a Intracellular free IC50 was calculated on the basis of intracellular free concentrations obtained from nominal concentrations times Kpuu at the corresponding concentration.