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Assay Detail

CHEMBL3039489

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ADMET
pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B1-transfected CHO cells
67
Total Activities
67
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
IC50 67 5.76 6.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1491099 GANGALEOIDIN 1 6.99
CHEMBL1328088 LEOIDIN 1 6.84
CHEMBL1171146 SARSASAPOGENIN 1 6.61
CHEMBL191 LOSARTAN 4.0 1 6.54
CHEMBL1489769 LASALOCID A SODIUM 1 6.32
CHEMBL230006 ENOXOLONE 2.0 1 6.28
CHEMBL15594 ARACHIDONIC ACID -1.0 1 6.22
CHEMBL1293 BETA CAROTENE 4.0 1 6.21
CHEMBL1200701 DICLOXACILLIN SODIUM 4.0 1 6.17
CHEMBL3039300 UTILIN 1 6.17
CHEMBL3039411 BUSSEIN 1 6.16
CHEMBL551842 LOBARIC ACID 1 6.14
CHEMBL1014 CANDESARTAN CILEXETIL 4.0 1 6.14
CHEMBL3039293 CHUKRASIN METHYL ETHER 1 6.12
CHEMBL3138689 1 6.09
CHEMBL393220 ATORVASTATIN CALCIUM 4.0 1 6.09
CHEMBL1200467 HYDROXYZINE PAMOATE 4.0 1 6.09
CHEMBL3138678 1 6.06
CHEMBL3138660 1 6.03
CHEMBL1200692 OLMESARTAN MEDOXOMIL 4.0 1 6.01
CHEMBL3138712 1 6.01
CHEMBL1603825 SCANDENIN 1 5.97
CHEMBL228281 NORSTICTIC ACID 1 5.94
CHEMBL1314749 DECAHYDROGAMBOGIC ACID 1 5.94
CHEMBL1456870 GARCINOLIC ACID 1 5.93
CHEMBL501680 BILIRUBIN 1.0 1 5.88
CHEMBL504794 beta-ESCIN 1 5.85
CHEMBL2269376 METHYL 6-ACETOXYANGOLENSATE 1 5.84
CHEMBL3138711 1 5.82
CHEMBL3138694 1 5.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1491099 GANGALEOIDIN IC50 = 102.33 nM 6.99
CHEMBL1328088 LEOIDIN IC50 = 144.54 nM 6.84
CHEMBL1171146 SARSASAPOGENIN IC50 = 245.47 nM 6.61
CHEMBL191 LOSARTAN IC50 = 288.4 nM 6.54
CHEMBL1489769 LASALOCID A SODIUM IC50 = 478.63 nM 6.32
CHEMBL230006 ENOXOLONE IC50 = 524.81 nM 6.28
CHEMBL15594 ARACHIDONIC ACID IC50 = 602.56 nM 6.22
CHEMBL1293 BETA CAROTENE IC50 = 616.6 nM 6.21
CHEMBL1200701 DICLOXACILLIN SODIUM IC50 = 676.08 nM 6.17
CHEMBL3039300 UTILIN IC50 = 676.08 nM 6.17
CHEMBL3039411 BUSSEIN IC50 = 691.83 nM 6.16
CHEMBL551842 LOBARIC ACID IC50 = 724.44 nM 6.14
CHEMBL1014 CANDESARTAN CILEXETIL IC50 = 724.44 nM 6.14
CHEMBL3039293 CHUKRASIN METHYL ETHER IC50 = 758.58 nM 6.12
CHEMBL1200467 HYDROXYZINE PAMOATE IC50 = 812.83 nM 6.09
CHEMBL393220 ATORVASTATIN CALCIUM IC50 = 812.83 nM 6.09
CHEMBL3138689 IC50 = 812.83 nM 6.09
CHEMBL3138678 IC50 = 870.96 nM 6.06
CHEMBL3138660 IC50 = 933.25 nM 6.03
CHEMBL1200692 OLMESARTAN MEDOXOMIL IC50 = 977.24 nM 6.01
CHEMBL3138712 IC50 = 977.24 nM 6.01
CHEMBL1603825 SCANDENIN IC50 = 1071.52 nM 5.97
CHEMBL228281 NORSTICTIC ACID IC50 = 1148.15 nM 5.94
CHEMBL1314749 DECAHYDROGAMBOGIC ACID IC50 = 1148.15 nM 5.94
CHEMBL1456870 GARCINOLIC ACID IC50 = 1174.9 nM 5.93
CHEMBL501680 BILIRUBIN IC50 = 1318.26 nM 5.88
CHEMBL504794 beta-ESCIN IC50 = 1412.54 nM 5.85
CHEMBL2269376 METHYL 6-ACETOXYANGOLENSATE IC50 = 1445.44 nM 5.84
CHEMBL3138711 IC50 = 1513.56 nM 5.82
CHEMBL3138694 IC50 = 1584.89 nM 5.80
CHEMBL464958 beta-DIHYDROGEDUNOL IC50 = 1698.24 nM 5.77
CHEMBL1017 TELMISARTAN IC50 = 1862.09 nM 5.73
CHEMBL1697717 CARBENOXOLONE SODIUM IC50 = 1949.84 nM 5.71
CHEMBL3137741 IC50 = 1995.26 nM 5.70
CHEMBL3138701 IC50 = 2187.76 nM 5.66
CHEMBL1526240 DIHYDROGAMBOGIC ACID IC50 = 2238.72 nM 5.65
CHEMBL486193 GILRETINOL ACETATE IC50 = 2238.72 nM 5.65
CHEMBL1436860 DIMETHYL GAMBOGATE IC50 = 2290.87 nM 5.64
CHEMBL3085392 PRIEURIANIN IC50 = 2344.23 nM 5.63
CHEMBL3138652 IC50 = 2398.83 nM 5.62
CHEMBL210868 AURIN IC50 = 2630.27 nM 5.58
CHEMBL506247 TANNIC ACID IC50 = 2630.27 nM 5.58
CHEMBL71893 ABIETIC ACID IC50 = 2691.53 nM 5.57
CHEMBL434864 THEAFLAVIN DIGALLATE IC50 = 2754.23 nM 5.56
CHEMBL1161 MOMETASONE FUROATE IC50 = 2951.21 nM 5.53
CHEMBL1200688 ERYTHROMYCIN ETHYLSUCCINATE IC50 = 3019.95 nM 5.52
CHEMBL3039417 ANTHOTHECOL IC50 = 3019.95 nM 5.52
CHEMBL1741 CLARITHROMYCIN IC50 = 3090.3 nM 5.51
CHEMBL51483 GOSSYPOL IC50 = 3235.94 nM 5.49
CHEMBL1751 DIGOXIN IC50 = 3235.94 nM 5.49