Assay Detail
ADMET
CHEMBL4011674
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Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay
72
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 72 | 7.35 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL472 | GLYBURIDE | 4.0 | 1 | 7.85 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.74 |
| CHEMBL1200624 | ETHYNODIOL DIACETATE | 4.0 | 1 | 7.70 |
| CHEMBL623 | NEFAZODONE | 4.0 | 1 | 7.50 |
| CHEMBL409 | BICALUTAMIDE | 4.0 | 1 | 7.31 |
| CHEMBL547 | ISOTRETINOIN | 4.0 | 1 | 7.31 |
| CHEMBL408 | TROGLITAZONE | 4.0 | 1 | 7.27 |
| CHEMBL806 | FLUTAMIDE | 4.0 | 1 | 7.24 |
| CHEMBL603 | ZAFIRLUKAST | 4.0 | 1 | 7.18 |
| CHEMBL2218877 | ERYTHROMYCIN ESTOLATE | 4.0 | 1 | 7.18 |
| CHEMBL1017 | TELMISARTAN | 4.0 | 1 | 7.15 |
| CHEMBL157101 | KETOCONAZOLE | 4.0 | 1 | 7.09 |
| CHEMBL1479 | DANAZOL | 4.0 | 1 | 7.06 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | - |
| CHEMBL621 | TRAZODONE | 4.0 | 1 | - |
| CHEMBL584 | NELFINAVIR | 4.0 | 1 | - |
| CHEMBL139 | DICLOFENAC | 4.0 | 1 | - |
| CHEMBL957 | BOSENTAN | 4.0 | 1 | - |
| CHEMBL714 | ALBUTEROL | 4.0 | 1 | - |
| CHEMBL388590 | BENZBROMARONE | 4.0 | 1 | - |
| CHEMBL54349 | ALPIDEM | 4.0 | 1 | - |
| CHEMBL422 | TRIFLUOPERAZINE | 4.0 | 1 | - |
| CHEMBL1064 | SIMVASTATIN | 4.0 | 1 | - |
| CHEMBL114 | SAQUINAVIR | 4.0 | 1 | - |
| CHEMBL444633 | RIFABUTIN | 4.0 | 1 | - |
| CHEMBL595 | PIOGLITAZONE | 4.0 | 1 | - |
| CHEMBL1726 | NISOLDIPINE | 4.0 | 1 | - |
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | - |
| CHEMBL1484 | NICARDIPINE | 4.0 | 1 | - |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL472 | GLYBURIDE | IC50 | = | 14.24 | nM | 7.85 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 18.39 | nM | 7.74 |
| CHEMBL1200624 | ETHYNODIOL DIACETATE | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL623 | NEFAZODONE | IC50 | = | 31.97 | nM | 7.50 |
| CHEMBL409 | BICALUTAMIDE | IC50 | = | 48.9 | nM | 7.31 |
| CHEMBL547 | ISOTRETINOIN | IC50 | = | 49.4 | nM | 7.31 |
| CHEMBL408 | TROGLITAZONE | IC50 | = | 53.2 | nM | 7.27 |
| CHEMBL806 | FLUTAMIDE | IC50 | = | 57.6 | nM | 7.24 |
| CHEMBL603 | ZAFIRLUKAST | IC50 | = | 66.2 | nM | 7.18 |
| CHEMBL2218877 | ERYTHROMYCIN ESTOLATE | IC50 | = | 65.8 | nM | 7.18 |
| CHEMBL1017 | TELMISARTAN | IC50 | = | 70.5 | nM | 7.15 |
| CHEMBL157101 | KETOCONAZOLE | IC50 | = | 80.6 | nM | 7.09 |
| CHEMBL1479 | DANAZOL | IC50 | = | 87.5 | nM | 7.06 |
| CHEMBL686 | MEFENAMIC ACID | IC50 | > | 100.0 | nM | - |
| CHEMBL841 | LOPERAMIDE | IC50 | - | — | - | |
| CHEMBL428647 | PACLITAXEL | IC50 | - | — | - | |
| CHEMBL103 | PROGESTERONE | IC50 | > | 100.0 | nM | - |
| CHEMBL374478 | RIFAMPIN | IC50 | - | — | - | |
| CHEMBL163 | RITONAVIR | IC50 | - | — | - | |
| CHEMBL121 | ROSIGLITAZONE | IC50 | > | 100.0 | nM | - |
| CHEMBL437765 | RIFAMYCIN | IC50 | - | — | - | |
| CHEMBL1136 | TELITHROMYCIN | IC50 | - | — | - | |
| CHEMBL160 | CYCLOSPORINE | IC50 | > | 100.0 | nM | - |
| CHEMBL832 | SULFINPYRAZONE | IC50 | - | — | - | |
| CHEMBL1159650 | CLOBETASOL PROPIONATE | IC50 | - | — | - | |
| CHEMBL926 | DOBUTAMINE | IC50 | - | — | - | |
| CHEMBL808 | ECONAZOLE | IC50 | > | 100.0 | nM | - |
| CHEMBL710 | FINASTERIDE | IC50 | - | — | - | |
| CHEMBL407 | FLUMAZENIL | IC50 | - | — | - | |
| CHEMBL1622 | FOLIC ACID | IC50 | - | — | - | |
| CHEMBL1544 | LIOTHYRONINE | IC50 | - | — | - | |
| CHEMBL54349 | ALPIDEM | IC50 | > | 100.0 | nM | - |
| CHEMBL49 | BUSPIRONE | IC50 | - | — | - | |
| CHEMBL1484 | NICARDIPINE | IC50 | > | 100.0 | nM | - |
| CHEMBL193 | NIFEDIPINE | IC50 | - | — | - | |
| CHEMBL1726 | NISOLDIPINE | IC50 | - | — | - | |
| CHEMBL595 | PIOGLITAZONE | IC50 | > | 100.0 | nM | - |
| CHEMBL444633 | RIFABUTIN | IC50 | - | — | - | |
| CHEMBL114 | SAQUINAVIR | IC50 | - | — | - | |
| CHEMBL1064 | SIMVASTATIN | IC50 | > | 100.0 | nM | - |
| CHEMBL422 | TRIFLUOPERAZINE | IC50 | - | — | - | |
| CHEMBL554 | LAPATINIB | IC50 | - | — | - | |
| CHEMBL388590 | BENZBROMARONE | IC50 | > | 100.0 | nM | - |
| CHEMBL714 | ALBUTEROL | IC50 | - | — | - | |
| CHEMBL957 | BOSENTAN | IC50 | > | 100.0 | nM | - |
| CHEMBL139 | DICLOFENAC | IC50 | > | 100.0 | nM | - |
| CHEMBL584 | NELFINAVIR | IC50 | > | 100.0 | nM | - |
| CHEMBL621 | TRAZODONE | IC50 | - | — | - | |
| CHEMBL941 | IMATINIB | IC50 | - | — | - | |
| CHEMBL5483011 | INDINAVIR | IC50 | - | — | - |