TABLE 3

PF-06649298 and PF-06761281 are potent inhibitors but low-affinity substrates

EC50 agonist mode membrane potential (μM)
CitrateSuccinatePF-06649298PF-06761281
216 ± 131018 ± 275N.D.4 ± 2
IC50 antagonist mode membrane potential (μM)
CitrateSuccinatePF-06649298PF-06761281
N.D.N.D.0.74 ± 0.230.36 ± 0.05
  • N.D., not determined. Data are averages ± S.E.M. from three independent experiments.