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Assay Detail

CHEMBL3039493

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ADMET
Ki values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells
67
Total Activities
66
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Cricetulus griseus
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Autocuration

Publication

Structure-based identification of OATP1B1/3 inhibitors.
De Bruyn T, van Westen GJ, Ijzerman AP, Stieger B, de Witte P, Augustijns PF, Annaert PP.
Mol Pharmacol (2013) 83 : 1257 -1267
PubMed 23571415 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 67 5.72 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1171146 SARSASAPOGENIN 1 7.10
CHEMBL228281 NORSTICTIC ACID 1 6.38
CHEMBL230006 ENOXOLONE 2.0 1 6.38
CHEMBL1255855 OLIGOMYCIN 1 6.36
CHEMBL3039411 BUSSEIN 1 6.28
CHEMBL1603825 SCANDENIN 1 6.25
CHEMBL3039293 CHUKRASIN METHYL ETHER 1 6.25
CHEMBL1489769 LASALOCID A SODIUM 1 6.23
CHEMBL3039300 UTILIN 1 6.22
CHEMBL486400 HEDERAGENIN 1 6.17
CHEMBL1200692 OLMESARTAN MEDOXOMIL 4.0 1 6.12
CHEMBL15594 ARACHIDONIC ACID -1.0 1 6.09
CHEMBL1161 MOMETASONE FUROATE 4.0 1 6.06
CHEMBL191 LOSARTAN 4.0 1 6.05
CHEMBL1200467 HYDROXYZINE PAMOATE 4.0 1 6.03
CHEMBL1017 TELMISARTAN 4.0 1 6.02
CHEMBL3138689 1 5.97
CHEMBL551842 LOBARIC ACID 1 5.90
CHEMBL1697717 CARBENOXOLONE SODIUM -1.0 1 5.83
CHEMBL1200701 DICLOXACILLIN SODIUM 4.0 1 5.81
CHEMBL1200688 ERYTHROMYCIN ETHYLSUCCINATE 4.0 1 5.79
CHEMBL1456870 GARCINOLIC ACID 1 5.76
CHEMBL1314749 DECAHYDROGAMBOGIC ACID 1 5.75
CHEMBL1328088 LEOIDIN 1 5.74
CHEMBL1014 CANDESARTAN CILEXETIL 4.0 1 5.72
CHEMBL1491099 GANGALEOIDIN 1 5.70
CHEMBL3137741 1 5.67
CHEMBL1293 BETA CAROTENE 4.0 1 5.65
CHEMBL1526240 DIHYDROGAMBOGIC ACID 1 5.65
CHEMBL3138712 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1171146 SARSASAPOGENIN Ki = 80.0 nM 7.10
CHEMBL230006 ENOXOLONE Ki = 420.0 nM 6.38
CHEMBL228281 NORSTICTIC ACID Ki = 420.0 nM 6.38
CHEMBL1255855 OLIGOMYCIN Ki = 440.0 nM 6.36
CHEMBL3039411 BUSSEIN Ki = 530.0 nM 6.28
CHEMBL3039293 CHUKRASIN METHYL ETHER Ki = 560.0 nM 6.25
CHEMBL1603825 SCANDENIN Ki = 560.0 nM 6.25
CHEMBL1489769 LASALOCID A SODIUM Ki = 590.0 nM 6.23
CHEMBL3039300 UTILIN Ki = 600.0 nM 6.22
CHEMBL486400 HEDERAGENIN Ki = 680.0 nM 6.17
CHEMBL1200692 OLMESARTAN MEDOXOMIL Ki = 750.0 nM 6.12
CHEMBL15594 ARACHIDONIC ACID Ki = 820.0 nM 6.09
CHEMBL1161 MOMETASONE FUROATE Ki = 870.0 nM 6.06
CHEMBL191 LOSARTAN Ki = 890.0 nM 6.05
CHEMBL1200467 HYDROXYZINE PAMOATE Ki = 940.0 nM 6.03
CHEMBL1017 TELMISARTAN Ki = 960.0 nM 6.02
CHEMBL3138689 Ki = 1080.0 nM 5.97
CHEMBL551842 LOBARIC ACID Ki = 1250.0 nM 5.90
CHEMBL1697717 CARBENOXOLONE SODIUM Ki = 1480.0 nM 5.83
CHEMBL1200701 DICLOXACILLIN SODIUM Ki = 1550.0 nM 5.81
CHEMBL1200688 ERYTHROMYCIN ETHYLSUCCINATE Ki = 1610.0 nM 5.79
CHEMBL1456870 GARCINOLIC ACID Ki = 1730.0 nM 5.76
CHEMBL1314749 DECAHYDROGAMBOGIC ACID Ki = 1770.0 nM 5.75
CHEMBL1328088 LEOIDIN Ki = 1840.0 nM 5.74
CHEMBL1014 CANDESARTAN CILEXETIL Ki = 1900.0 nM 5.72
CHEMBL1491099 GANGALEOIDIN Ki = 2020.0 nM 5.70
CHEMBL3137741 Ki = 2160.0 nM 5.67
CHEMBL1293 BETA CAROTENE Ki = 2260.0 nM 5.65
CHEMBL1526240 DIHYDROGAMBOGIC ACID Ki = 2240.0 nM 5.65
CHEMBL3138712 Ki = 2270.0 nM 5.64
CHEMBL2218877 ERYTHROMYCIN ESTOLATE Ki = 2350.0 nM 5.63
CHEMBL3138693 Ki = 2390.0 nM 5.62
CHEMBL3138693 Ki = 2500.0 nM 5.60
CHEMBL393220 ATORVASTATIN CALCIUM Ki = 2580.0 nM 5.59
CHEMBL3138664 Ki = 2550.0 nM 5.59
CHEMBL3039417 ANTHOTHECOL Ki = 2640.0 nM 5.58
CHEMBL501680 BILIRUBIN Ki = 2630.0 nM 5.58
CHEMBL3085392 PRIEURIANIN Ki = 2630.0 nM 5.58
CHEMBL504794 beta-ESCIN Ki = 2610.0 nM 5.58
CHEMBL1255589 LORGLUMIDE SODIUM Ki = 2710.0 nM 5.57
CHEMBL3039264 3-DEOXO-3beta-ACETOXYDEOXYDIHYDROGEDUNIN Ki = 2670.0 nM 5.57
CHEMBL3138711 Ki = 2890.0 nM 5.54
CHEMBL3138701 Ki = 2890.0 nM 5.54
CHEMBL1078052 CHOLIC ACID, METHYL ESTER Ki = 2890.0 nM 5.54
CHEMBL1410 NONOXYNOL 9 Ki = 2870.0 nM 5.54
CHEMBL2269376 METHYL 6-ACETOXYANGOLENSATE Ki = 2920.0 nM 5.54
CHEMBL44 GENISTEIN Ki = 2960.0 nM 5.53
CHEMBL3138678 Ki = 3050.0 nM 5.52
CHEMBL3138642 Ki = 3060.0 nM 5.51
CHEMBL210868 AURIN Ki = 3150.0 nM 5.50