Assay Detail
Binding
CHEMBL3540573
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human 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 | Homo sapiens |
| 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 | 5.05 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | 6.52 |
| CHEMBL160 | CYCLOSPORINE | 4.0 | 1 | 6.30 |
| CHEMBL408 | TROGLITAZONE | 4.0 | 1 | 5.57 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 5.54 |
| CHEMBL2218877 | ERYTHROMYCIN ESTOLATE | 4.0 | 1 | 5.39 |
| CHEMBL623 | NEFAZODONE | 4.0 | 1 | 5.38 |
| CHEMBL472 | GLYBURIDE | 4.0 | 1 | 5.28 |
| CHEMBL437765 | RIFAMYCIN | 4.0 | 1 | 5.20 |
| CHEMBL121 | ROSIGLITAZONE | 4.0 | 1 | 5.19 |
| CHEMBL1159650 | CLOBETASOL PROPIONATE | 4.0 | 1 | 5.07 |
| CHEMBL54349 | ALPIDEM | 4.0 | 1 | 5.04 |
| CHEMBL374478 | RIFAMPIN | 4.0 | 1 | 4.95 |
| CHEMBL374975 | FUSIDIC ACID | 3.0 | 1 | 4.94 |
| CHEMBL1131 | ACITRETIN | 4.0 | 1 | 4.74 |
| CHEMBL146095 | GLAFENINE | 4.0 | 1 | 4.65 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 4.51 |
| CHEMBL957 | BOSENTAN | 4.0 | 1 | 4.42 |
| CHEMBL893 | DICLOXACILLIN | 4.0 | 1 | 4.16 |
| CHEMBL833 | TICLOPIDINE | 4.0 | 1 | 4.13 |
| CHEMBL976 | PRAZIQUANTEL | 4.0 | 1 | 4.01 |
| CHEMBL1515 | METHIMAZOLE | 4.0 | 1 | - |
| CHEMBL112 | ACETAMINOPHEN | 4.0 | 1 | - |
| CHEMBL26 | SULPIRIDE | 3.0 | 1 | - |
| CHEMBL15770 | SULINDAC | 4.0 | 1 | - |
| CHEMBL1542 | AZATHIOPRINE | 4.0 | 1 | - |
| CHEMBL340978 | BENOXAPROFEN | 4.0 | 1 | - |
| CHEMBL264374 | BEZAFIBRATE | 3.0 | 1 | - |
| CHEMBL1790041 | RANITIDINE | 4.0 | 1 | - |
| CHEMBL273575 | NOMIFENSINE | 4.0 | 1 | - |
| CHEMBL572 | NITROFURANTOIN | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL595 | PIOGLITAZONE | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL160 | CYCLOSPORINE | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL408 | TROGLITAZONE | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL2218877 | ERYTHROMYCIN ESTOLATE | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL623 | NEFAZODONE | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL472 | GLYBURIDE | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL437765 | RIFAMYCIN | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL121 | ROSIGLITAZONE | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL1159650 | CLOBETASOL PROPIONATE | IC50 | = | 8500.0 | nM | 5.07 |
| CHEMBL54349 | ALPIDEM | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL374478 | RIFAMPIN | IC50 | = | 11300.0 | nM | 4.95 |
| CHEMBL374975 | FUSIDIC ACID | IC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL1131 | ACITRETIN | IC50 | = | 18200.0 | nM | 4.74 |
| CHEMBL146095 | GLAFENINE | IC50 | = | 22300.0 | nM | 4.65 |
| CHEMBL193 | NIFEDIPINE | IC50 | = | 30700.0 | nM | 4.51 |
| CHEMBL957 | BOSENTAN | IC50 | = | 38100.0 | nM | 4.42 |
| CHEMBL893 | DICLOXACILLIN | IC50 | = | 69700.0 | nM | 4.16 |
| CHEMBL833 | TICLOPIDINE | IC50 | = | 74000.0 | nM | 4.13 |
| CHEMBL976 | PRAZIQUANTEL | IC50 | = | 96800.0 | nM | 4.01 |
| CHEMBL498 | CHLORPROPAMIDE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL557555 | CIPROFIBRATE | IC50 | = | 572700.0 | nM | - |
| CHEMBL806 | FLUTAMIDE | IC50 | = | 143200.0 | nM | - |
| CHEMBL222645 | FLOXACILLIN | IC50 | = | 208600.0 | nM | - |
| CHEMBL1909282 | FENCLOZIC ACID | IC50 | > | 1000000.0 | nM | - |
| CHEMBL902 | FAMOTIDINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL777 | CLAVULANIC ACID | IC50 | > | 1000000.0 | nM | - |
| CHEMBL1430 | PENICILLAMINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL891 | CLOXACILLIN | IC50 | = | 219700.0 | nM | - |
| CHEMBL1043 | DAPSONE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL407 | FLUMAZENIL | IC50 | > | 1000000.0 | nM | - |
| CHEMBL93 | ZILEUTON | IC50 | > | 1000000.0 | nM | - |
| CHEMBL1082 | AMOXICILLIN | IC50 | > | 1000000.0 | nM | - |
| CHEMBL95889 | BETAINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL49 | BUSPIRONE | IC50 | = | 104500.0 | nM | - |
| CHEMBL521 | IBUPROFEN | IC50 | = | 598600.0 | nM | - |
| CHEMBL92401 | IPRONIAZID | IC50 | > | 1000000.0 | nM | - |
| CHEMBL71 | CHLORPROMAZINE | IC50 | = | 147600.0 | nM | - |
| CHEMBL42 | CLOZAPINE | IC50 | = | 126100.0 | nM | - |
| CHEMBL108 | CARBAMAZEPINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL572 | NITROFURANTOIN | IC50 | > | 1000000.0 | nM | - |
| CHEMBL273575 | NOMIFENSINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL1790041 | RANITIDINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL264374 | BEZAFIBRATE | IC50 | = | 231700.0 | nM | - |
| CHEMBL340978 | BENOXAPROFEN | IC50 | = | 175000.0 | nM | - |
| CHEMBL1542 | AZATHIOPRINE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL15770 | SULINDAC | IC50 | = | 226000.0 | nM | - |
| CHEMBL26 | SULPIRIDE | IC50 | > | 1000000.0 | nM | - |
| CHEMBL112 | ACETAMINOPHEN | IC50 | > | 1000000.0 | nM | - |
| CHEMBL1515 | METHIMAZOLE | IC50 | > | 1000000.0 | nM | - |