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Assay Detail

CHEMBL3039492

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ADMET
pIC50 values for sodium fluorescein (10 uM) uptake in OATP1B3-transfected CHO cells
66
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
IC50 66 5.58 6.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1171146 SARSASAPOGENIN 1 6.98
CHEMBL230006 ENOXOLONE 2.0 1 6.26
CHEMBL228281 NORSTICTIC ACID 1 6.26
CHEMBL3039411 BUSSEIN 1 6.16
CHEMBL3039293 CHUKRASIN METHYL ETHER 1 6.14
CHEMBL1603825 SCANDENIN 1 6.13
CHEMBL1489769 LASALOCID A SODIUM 1 6.11
CHEMBL3039300 UTILIN 1 6.11
CHEMBL486400 HEDERAGENIN 1 6.05
CHEMBL1200692 OLMESARTAN MEDOXOMIL 4.0 1 6.01
CHEMBL15594 ARACHIDONIC ACID -1.0 1 5.97
CHEMBL191 LOSARTAN 4.0 1 5.94
CHEMBL1161 MOMETASONE FUROATE 4.0 1 5.94
CHEMBL1200467 HYDROXYZINE PAMOATE 4.0 1 5.91
CHEMBL1017 TELMISARTAN 4.0 1 5.90
CHEMBL3138689 1 5.85
CHEMBL551842 LOBARIC ACID 1 5.79
CHEMBL1697717 CARBENOXOLONE SODIUM -1.0 1 5.72
CHEMBL1200701 DICLOXACILLIN SODIUM 4.0 1 5.70
CHEMBL1200688 ERYTHROMYCIN ETHYLSUCCINATE 4.0 1 5.68
CHEMBL1456870 GARCINOLIC ACID 1 5.65
CHEMBL1314749 DECAHYDROGAMBOGIC ACID 1 5.64
CHEMBL1328088 LEOIDIN 1 5.62
CHEMBL1014 CANDESARTAN CILEXETIL 4.0 1 5.61
CHEMBL1491099 GANGALEOIDIN 1 5.58
CHEMBL3137741 1 5.55
CHEMBL1526240 DIHYDROGAMBOGIC ACID 1 5.54
CHEMBL3138712 1 5.53
CHEMBL1293 BETA CAROTENE 4.0 1 5.53
CHEMBL3138694 1 5.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1171146 SARSASAPOGENIN IC50 = 104.71 nM 6.98
CHEMBL230006 ENOXOLONE IC50 = 549.54 nM 6.26
CHEMBL228281 NORSTICTIC ACID IC50 = 549.54 nM 6.26
CHEMBL3039411 BUSSEIN IC50 = 691.83 nM 6.16
CHEMBL3039293 CHUKRASIN METHYL ETHER IC50 = 724.44 nM 6.14
CHEMBL1603825 SCANDENIN IC50 = 741.31 nM 6.13
CHEMBL1489769 LASALOCID A SODIUM IC50 = 776.25 nM 6.11
CHEMBL3039300 UTILIN IC50 = 776.25 nM 6.11
CHEMBL486400 HEDERAGENIN IC50 = 891.25 nM 6.05
CHEMBL1200692 OLMESARTAN MEDOXOMIL IC50 = 977.24 nM 6.01
CHEMBL15594 ARACHIDONIC ACID IC50 = 1071.52 nM 5.97
CHEMBL191 LOSARTAN IC50 = 1148.15 nM 5.94
CHEMBL1161 MOMETASONE FUROATE IC50 = 1148.15 nM 5.94
CHEMBL1200467 HYDROXYZINE PAMOATE IC50 = 1230.27 nM 5.91
CHEMBL1017 TELMISARTAN IC50 = 1258.93 nM 5.90
CHEMBL3138689 IC50 = 1412.54 nM 5.85
CHEMBL551842 LOBARIC ACID IC50 = 1621.81 nM 5.79
CHEMBL1697717 CARBENOXOLONE SODIUM IC50 = 1905.46 nM 5.72
CHEMBL1200701 DICLOXACILLIN SODIUM IC50 = 1995.26 nM 5.70
CHEMBL1200688 ERYTHROMYCIN ETHYLSUCCINATE IC50 = 2089.3 nM 5.68
CHEMBL1456870 GARCINOLIC ACID IC50 = 2238.72 nM 5.65
CHEMBL1314749 DECAHYDROGAMBOGIC ACID IC50 = 2290.87 nM 5.64
CHEMBL1328088 LEOIDIN IC50 = 2398.83 nM 5.62
CHEMBL1014 CANDESARTAN CILEXETIL IC50 = 2454.71 nM 5.61
CHEMBL1491099 GANGALEOIDIN IC50 = 2630.27 nM 5.58
CHEMBL3137741 IC50 = 2818.38 nM 5.55
CHEMBL1526240 DIHYDROGAMBOGIC ACID IC50 = 2884.03 nM 5.54
CHEMBL3138712 IC50 = 2951.21 nM 5.53
CHEMBL1293 BETA CAROTENE IC50 = 2951.21 nM 5.53
CHEMBL3138694 IC50 = 2951.21 nM 5.53
CHEMBL2218877 ERYTHROMYCIN ESTOLATE IC50 = 3090.3 nM 5.51
CHEMBL464958 beta-DIHYDROGEDUNOL IC50 = 3235.94 nM 5.49
CHEMBL3138664 IC50 = 3311.31 nM 5.48
CHEMBL1741 CLARITHROMYCIN IC50 = 3311.31 nM 5.48
CHEMBL501680 BILIRUBIN IC50 = 3388.44 nM 5.47
CHEMBL393220 ATORVASTATIN CALCIUM IC50 = 3388.44 nM 5.47
CHEMBL504794 beta-ESCIN IC50 = 3388.44 nM 5.47
CHEMBL3085392 PRIEURIANIN IC50 = 3388.44 nM 5.47
CHEMBL3039417 ANTHOTHECOL IC50 = 3467.37 nM 5.46
CHEMBL1410 NONOXYNOL 9 IC50 = 3715.35 nM 5.43
CHEMBL3138701 IC50 = 3715.35 nM 5.43
CHEMBL1078052 CHOLIC ACID, METHYL ESTER IC50 = 3715.35 nM 5.43
CHEMBL2269376 METHYL 6-ACETOXYANGOLENSATE IC50 = 3801.89 nM 5.42
CHEMBL3138711 IC50 = 3801.89 nM 5.42
CHEMBL44 GENISTEIN IC50 = 3890.45 nM 5.41
CHEMBL3138678 IC50 = 3981.07 nM 5.40
CHEMBL210868 AURIN IC50 = 4073.8 nM 5.39
CHEMBL506247 TANNIC ACID IC50 = 4168.69 nM 5.38
CHEMBL9509 SILIBININ IC50 = 4265.8 nM 5.37
CHEMBL36327 EPICATECHIN GALLATE IC50 = 4466.84 nM 5.35