Assay Detail
Binding
CHEMBL3540574
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake
85
Total Activities
85
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | Sf21 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 85 | 4.73 | 6.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 6.22 |
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | 5.70 |
| CHEMBL472 | GLYBURIDE | 4.0 | 1 | 5.55 |
| CHEMBL437765 | RIFAMYCIN | 4.0 | 1 | 5.51 |
| CHEMBL408 | TROGLITAZONE | 4.0 | 1 | 4.97 |
| CHEMBL2218877 | ERYTHROMYCIN ESTOLATE | 4.0 | 1 | 4.94 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 4.81 |
| CHEMBL623 | NEFAZODONE | 4.0 | 1 | 4.76 |
| CHEMBL374975 | FUSIDIC ACID | 3.0 | 1 | 4.76 |
| CHEMBL1131 | ACITRETIN | 4.0 | 1 | 4.71 |
| CHEMBL54349 | ALPIDEM | 4.0 | 1 | 4.64 |
| CHEMBL957 | BOSENTAN | 4.0 | 1 | 4.51 |
| CHEMBL146095 | GLAFENINE | 4.0 | 1 | 4.49 |
| CHEMBL1159650 | CLOBETASOL PROPIONATE | 4.0 | 1 | 4.46 |
| CHEMBL374478 | RIFAMPIN | 4.0 | 1 | 4.46 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 4.40 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 4.34 |
| CHEMBL1324 | TOLCAPONE | 4.0 | 1 | 4.33 |
| CHEMBL833 | TICLOPIDINE | 4.0 | 1 | 4.31 |
| CHEMBL806 | FLUTAMIDE | 4.0 | 1 | 4.10 |
| CHEMBL15770 | SULINDAC | 4.0 | 1 | 4.06 |
| CHEMBL340978 | BENOXAPROFEN | 4.0 | 1 | 4.00 |
| CHEMBL1790041 | RANITIDINE | 4.0 | 1 | - |
| CHEMBL264374 | BEZAFIBRATE | 3.0 | 1 | - |
| CHEMBL572 | NITROFURANTOIN | 4.0 | 1 | - |
| CHEMBL273575 | NOMIFENSINE | 4.0 | 1 | - |
| CHEMBL92401 | IPRONIAZID | 2.0 | 1 | - |
| CHEMBL1542 | AZATHIOPRINE | 4.0 | 1 | - |
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | - |
| CHEMBL112 | ACETAMINOPHEN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL595 | PIOGLITAZONE | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL472 | GLYBURIDE | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL437765 | RIFAMYCIN | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL408 | TROGLITAZONE | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL2218877 | ERYTHROMYCIN ESTOLATE | IC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 15600.0 | nM | 4.81 |
| CHEMBL623 | NEFAZODONE | IC50 | = | 17400.0 | nM | 4.76 |
| CHEMBL374975 | FUSIDIC ACID | IC50 | = | 17400.0 | nM | 4.76 |
| CHEMBL1131 | ACITRETIN | IC50 | = | 19700.0 | nM | 4.71 |
| CHEMBL54349 | ALPIDEM | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL957 | BOSENTAN | IC50 | = | 30600.0 | nM | 4.51 |
| CHEMBL146095 | GLAFENINE | IC50 | = | 32200.0 | nM | 4.49 |
| CHEMBL1159650 | CLOBETASOL PROPIONATE | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL374478 | RIFAMPIN | IC50 | = | 34700.0 | nM | 4.46 |
| CHEMBL121 | ROSIGLITAZONE | IC50 | = | 40000.0 | nM | 4.40 |
| CHEMBL193 | NIFEDIPINE | IC50 | = | 45400.0 | nM | 4.34 |
| CHEMBL1324 | TOLCAPONE | IC50 | = | 47200.0 | nM | 4.33 |
| CHEMBL833 | TICLOPIDINE | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL806 | FLUTAMIDE | IC50 | = | 78700.0 | nM | 4.10 |
| CHEMBL15770 | SULINDAC | IC50 | = | 87500.0 | nM | 4.06 |
| CHEMBL340978 | BENOXAPROFEN | IC50 | = | 99100.0 | nM | 4.00 |
| CHEMBL1909282 | FENCLOZIC ACID | IC50 | > | 1000000.0 | nM | - |
| CHEMBL902 | FAMOTIDINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL498 | CHLORPROPAMIDE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL1430 | PENICILLAMINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL893 | DICLOXACILLIN | IC50 | = | 111100.0 | nM | - |
| CHEMBL1043 | DAPSONE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL557555 | CIPROFIBRATE | IC50 | = | 189900.0 | nM | - |
| CHEMBL42 | CLOZAPINE | IC50 | = | 196500.0 | nM | - |
| CHEMBL891 | CLOXACILLIN | IC50 | = | 376700.0 | nM | - |
| CHEMBL434 | ISOPROTERENOL | IC50 | > | 1000000.0 | nM | - |
| CHEMBL1082 | AMOXICILLIN | IC50 | > | 1000000.0 | nM | - |
| CHEMBL95889 | BETAINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL49 | BUSPIRONE | IC50 | = | 369800.0 | nM | - |
| CHEMBL428880 | CROMOLYN | IC50 | > | 1000000.0 | nM | - |
| CHEMBL222645 | FLOXACILLIN | IC50 | = | 429100.0 | nM | - |
| CHEMBL71 | CHLORPROMAZINE | IC50 | = | 122300.0 | nM | - |
| CHEMBL108 | CARBAMAZEPINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL521 | IBUPROFEN | IC50 | = | 290900.0 | nM | - |
| CHEMBL777 | CLAVULANIC ACID | IC50 | > | 1000000.0 | nM | - |
| CHEMBL1515 | METHIMAZOLE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL112 | ACETAMINOPHEN | IC50 | > | 1000000.0 | nM | - |
| CHEMBL26 | SULPIRIDE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL1542 | AZATHIOPRINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL92401 | IPRONIAZID | IC50 | > | 1000000.0 | nM | - |
| CHEMBL273575 | NOMIFENSINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL572 | NITROFURANTOIN | IC50 | > | 1000000.0 | nM | - |
| CHEMBL264374 | BEZAFIBRATE | IC50 | = | 391000.0 | nM | - |
| CHEMBL1790041 | RANITIDINE | IC50 | > | 1000000.0 | nM | - |