Table 2: Inhibition of OATP1B1- and OATP1B3-Mediated Fluorescein-Methotrexate (FMTX) Uptake by Prestwick Library Compounds

Compound IC50 on OATP1B1 (µM) IC50 on OATP1B3 (µM)
2-aminobenzenesulfonamide > 100 > 100
Aconitine > 100 No inhibition
Beclomethasone 6.7 ± 1.2 1.4 ± 0.4
Bromocryptine 0.7 ± 0.08 1.8 ± 0.3
Captopril No inhibition No inhibition
Ergocryptine 0.8 ± 0.2 2.2 ± 1.2
Estropipate 0.06 ± 0.01 19.3 ± 6.3
Etomidate > 100 > 100
Fipexide 34.5 ± 6.8 > 100
Metronidazole > 100 > 100
Moricizine 8.1 ± 1.9 2.7 ± 0.4
Niflumic acid 3.7 ± 1.4 22.0 ± 6.8
Ramipril 4.0 ± 0.5 3.3 ± 0.3
Repaglinide 1.1 ± 0.2 4.8 ± 0.7
Resveratrol 11.2 ± 2.0 23.7 ± 2.5
Rifampicin 1.3 ± 0.2 1.5 ± 0.5
Trifluridine No inhibition No inhibition
Ursolic acid 12.5 ± 1.9 2.3 ± 0.03

Results are means ± SE of at least three independent experiments.