TABLE 1

Inhibition of creatinine transport by INCB039110 or by a reference inhibitor

IC50 values in μM, mean ± S.D.; N = 3.

TransporterINCB039110Reference Inhibitor
OAT284 ± 30Indomethacin6.5 ± 1.1
OCT25.8 ± 2.0Cimetidine17 ± 3.3
OCT380 ± 28Quinidine150 ± 39
MATE1/MATE2-K3.7 ± 1.9Cimetidine4.6 ± 2.2
OAT2/OCT2/OCT3/MATE1/MATE2-K27 ± 7.0Cimetidine32 ± 7.1