TABLE 1

OATP1B inhibition data for all test compounds that inhibited sodium fluorescein uptake by at least 50%

CompoundSodium FluoresceinKi ValueCompoundSodium FluoresceinKi Value
OATP1B1OATP1B3OATP1B1OATP1B3OATP1B1OATP1B3OATP1B1OATP1B3
% of control% of controlµMµM% of control% of controlµMµM
Utilin−3.82.70.380.603β-Hydroxydeoxydesacetoxy-7-oxogedunin10.822.21.333.81
Entandrophragmin−0.40.6Norstictic acid10.91.80.630.42
Erythromycin ethylsuccinate3.630.51.671.61β-Escin11.011.70.782.61
Rosolic Acid4.120.41.433.15Oligomycin A11.33.00.250.44
Gangaleoidin4.115.00.062.02Dicloxacillin Sodium11.49.80.371.55
Cyclosporine4.64.26-Acetoxyangolensic acid methyl ester12.035.00.802.92
3α-Hydroxygedinin6.123.21.212.89Hydroxyzine pamoate12.213.60.450.94
Lithocholic acid6.660.2Tetrahydrogambogic acid12.54.41.102.16
Chukrasin, methyl ether6.83.80.420.561,2α-Epoxydeacetoxydihyrogedunin12.721.3
Erythromycin estolate6.97.42.412.35Decahydrogambogic acid12.818.20.621.77
Bussein7.35.40.380.53Theaflavin digallate13.19.41.513.42
Abietic acid7.433.81.474.08Ethinyl estradiol13.161.2
Hexachlorophene7.63.1Scandenin13.89.00.590.56
Leoidin7.814.60.081.843β-Acetoxydeoxyangolensic acid14.021.90.513.47
Rhodomyrtoxin B8.137.5Swietenine14.069.9
Deoxygedunin8.722.70.832.89Cephaloridine14.232.0
Chlormadinone acetate9.724.4Dihydrogambogic acid14.217.31.232.24
β-Carotene10.013.40.342.267-Deacetylkhivorin14.39.50.542.27
Lasalocid sodium10.36.70.260.59Bergenin14.694.5
Acetyl isogambogic acid10.430.32.244.173-Deoxo-3β-acetoxydeoxy-dihydrogedunin15.020.70.412.67
Candesartan cilextil10.66.00.401.90Bilirubin15.332.10.722.63
Olmesartan medoxomil15.49.70.540.75Diffratic acid22.712.7
Carbenoxolone sodium15.414.51.071.48Prieurianin22.825.51.282.63
19-Hydroxytotarol15.920.5Dihydrodeoxygedunin22.854.71.945.99
3α-Hydroxy-3-deoxy-angolensic acid16.017.50.683.06Baeomycesic acid23.046.8
Paclitaxel16.452.9Dimethyl gambogate23.262.11.263.94
Lorglumide sodium16.532.82.012.71Losartan23.23.80.160.89
Lobaric acid18.37.60.401.25Rotenone23.243.9
α-Dihydrogedunol18.332.2Deoxygedunol acetate23.349.2
Isogedunin18.646.9Arachidonic acid23.45.40.330.82
Tannic acid18.710.61.463.236-Hydroxyangolensic acid23.761.1
3α-Acetoxydihydro-deoxygedunin18.98.00.441.08Lithocholenic acid23.7112.0
Retinol19.032.0Morin24.245.4
Retinyl acetate19.423.51.223.89Dihydrocaryophyllenone24.239.1
11-Oxoursolic acid19.85.2Gossypol24.515.81.783.47
Pentachlorophenol20.040.7Chrysanthellin A25.117.41.824.02
Clobetasol propionate20.221.3Teniposide25.432.6
Angolensic acid20.333.7Betulinic acid25.938.6
Anthothecol20.412.41.652.64Khayanthone26.057.6
β-Dihydrogedunol20.523.80.932.5Cholic acid, methyl ester26.040.94.582.89
11α-Acetoxykhivorin20.646.10.483.05Carnosine26.498.9
Phenolphthalein20.638.0Lonchocarpic acid26.536.3
Suramin20.830.8Umbelliferone26.776.5
Carapin20.966.5Diltiazem hydrochloride26.780.8
Carminic acid21.6121.9Tretinon26.855.5
Salinomycin sodium21.717.02.033.31Bromo-3-hydroxy-4-succinylcaryolane26.850.1
Humilin A22.334.4Dihydroergotamine mesylate27.110.1
Xylocarpus A22.59.83-Deoxy-3β-hydroxymexicanolide 16-enol ether27.2106.5
Fissinolide27.451.8Isotretinon32.251.5
Violastyrene27.547.9N-(9-Fluorenylmethoxycarbonyl)-L-Leucine32.548.3
Deoxyandirobin27.742.8Dihydrogeduninic acid, methyl ester32.797.1
Androsterone sodium sulfate27.840.8Nonoxynol32.728.01.922.87
Prieuranin acetate28.254.4Dicumarol33.119.3
8β-Hydroxycarapin28.549.6Tetrac33.471.4
Euphol acetate29.240.21,7-Dideacetoxy-1,7-dioxo-3-deacetylkhivorin33.561.5
Deoxyandirobin lactone29.553.1Rifampicin33.622.0
2-Methylene-5-dioxotetrahydro-furanyl-6-oxodimethyl-bicycloundecane29.847.6Mometasone furoate34.025.61.620.87
Dihydromunduletone30.358.7Citrinin34.467.3
Cyproterone30.6112.26,4′-Dimethoxyflavone34.4110.4
Garcinolic acid30.63.60.651.73Ajmaline34.691.5
1,2α-Epoxydeoxy-dihydrogedunin30.838.60.862.28Gangleoidin acetate34.654.6
Usnic acid31.169.1Dihydrogedunin35.562.4
2,2-Bisepigallocatechin monogallate31.118.82.056.50Enoxolone35.64.30.290.42
1,3-Dideacetyldeoxy-khivorin31.150.82.966.49Amcinonide25.856.6
Iopanic acid31.159.6Atorvastatin calcium36.132.10.452.58
Rhodomyrtoxin31.166.2Bithionol36.137.2
Mundulone31.245.1Isoginkgetin36.263.5
Pyrantel pamoate31.434.8Proadifen HCl36.253.5
3β-Hydroxydeoxodihydro-deoxygedunin31.525.91.492.39Fludrocortisone acetate36.371.2
Ergosterol31.752.3Oleanolic acid acetate37.024.7
Antimycin A31.928.62.203.82Chenodiol37.971.6
Canrenone32.078.7α-Hyodeoxycholic acid38.289.1
Isoxsuprine HCl38.477.5Clomipramine HCl43.678.8
Isoreserpine38.542.2Budesonide43.873.0
6-oxoprogesterone38.575.5Mexicanolide44.1122.7
Betamethasone valerate38.610.2Simvastatin44.760.2
3,5-Dinitrocatechol38.675.4Cedrelone44.760.7
N-Formylmethionylphenyl-alanine28.8104.4Haematoporphyrin dihydrochloride45.040.1
Pectolinarin39.1155.8Cephalothin sodium45.166.3
2-Methyl gramine39.280.1Thyroxine45.267.3
Sildenafil39.3107.1Epicatechin monogallate46.425.32.073.46
Fusidic acid39.558.3Ginkgetin46.446.7
3β-Acetoxydeoxodihydro-gedunin39.6104.7Bacampicillin HCl46.480.6
5-Nitro-2-phenylpropyl-aminobenzoic acid40.133.4Hexestrol46.643.2
Hederagenin40.218.62.110.6818α-Glycyrrhetinic acid47.159.1
Deacetoxy-7-oxogedunin40.385.1Quercetin47.1122.7
Chol-11-enic acid40.4203.4Cloxacillin sodium47.363.2
Troleandomycin40.542.012-Hydroxy-4,4′-bisnor-podocarpatetraen-one47.582.2
Hydroxyprogesterone caproate40.655.8Dihydrocelastryl diacetate47.613.7
Allopregnanolone41.589.7Glycyrrhizic acid47.639.9
Beclomethasone dipropionate41.514.8Carprofen47.777.8
Hecogenin41.8105.1Boldine47.9100.1
Oxyphenbutazone42.083.2Tridesacetoxykhivorin48.084.2
Verapamil HCl42.189.2Methyl-7-deshydroxypyrogallin-4-carboxylate48.280.2
4′-Demethylepipodo-phyllotoxin42.569.61,3-Dideacetyl-7-deacetoxy-7-oxokhivorin48.293.9
Emetine42.665.6Solidagenone48.378.8
Pyrvinium pamoate42.632.7Epiafzelechin48.326.7
Azelastine HCl43.4134.9Alverine citrate48.374.4
Chloroxine43.562.2Aloin48.566.8
Larixol48.678.32,3-Diacetoxy-7,8-epoxy-24,29-dinor-1,3,5-friedelatriene-20-carboxylic acid63.637.7
Nicolsamide48.747.1Nimodipine64.837.8
Dienestrol48.761.9Genistein95.639.15.002.96
Asarylaldehyde48.759.2Dihydrocelasterol70.540.4
Acetylglucosamine49.083.0Telmisartan77.641.91.030.96
Epigallocatechin-3-monogallate49.045.9Sulfinpyrazone55.243.9
Guaiazulene49.150.3Diethylstilbestrol63.745.6
Loganic acid49.299.5Silibinin54.846.93.373.27
Nystatin49.276.2Novobiocin sodium56.247.2
Protoporphynyrinix49.694.6Irbesartan76.047.2
Suxibuzone49.684.7Dihydro-7-desacetyldeoxygedunin54.848.33.442.55
Digydrogedunic acid, methyl ester49.799.1Cosmosiin hexaacetate95.248.4
Coniferyl alcohol49.766.1Troxerutin61.949.5
Dextromethorphan HBr49.878.2
Rosuvastatin52.15.72.433.61
Glucosaminic acid63.525.6
Smilagenin50.825.70.130.08
Ergocalciferol81.728.8
Isopimpinellin84.529.0
Echinocystic acid69.330.5
Ezetimibe51.430.6
Stictic acid94.332.3
Madecassic acid69.333.8
Irigenin, 7-benzyl ether60.737.0