Assay Detail
ADMET
CHEMBL3531874
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Rattus norvegicus |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Nuclear receptor subfamily 1 group I member 2 (CHEMBL2146315) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Identification of clinically used drugs that activate pregnane X receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 36 | 5.25 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL94657 | PATUPILONE | 3.0 | 1 | 8.00 |
| CHEMBL312862 | DEMECOLCINE | 2.0 | 1 | 7.05 |
| CHEMBL1237054 | PLICAMYCIN | 4.0 | 1 | 6.50 |
| CHEMBL1200600 | FLUOROMETHOLONE | 4.0 | 1 | 6.40 |
| CHEMBL542541 | HYDRALAZINE HYDROCHLORIDE | 4.0 | 1 | 6.35 |
| CHEMBL1200617 | RIMEXOLONE | 4.0 | 1 | 6.17 |
| CHEMBL1891684 | RIODIPINE | 2.0 | 1 | 5.75 |
| CHEMBL98 | VORINOSTAT | 4.0 | 1 | 5.60 |
| CHEMBL384467 | DEXAMETHASONE | 4.0 | 1 | 5.58 |
| CHEMBL474260 | CARUBICIN | 2.0 | 1 | 5.55 |
| CHEMBL650 | METHYLPREDNISOLONE | 4.0 | 1 | 5.40 |
| CHEMBL37161 | FENBENDAZOLE | 2.0 | 1 | 5.40 |
| CHEMBL1530428 | DEXAMETHASONE ACETATE | 4.0 | 1 | 5.35 |
| CHEMBL1702784 | — | — | 1 | 5.35 |
| CHEMBL52606 | COLFORSIN | 2.0 | 1 | 5.15 |
| CHEMBL284733 | DICLAZURIL | 2.0 | 1 | 5.05 |
| CHEMBL1714574 | TERCONAZOLE | 4.0 | 1 | 5.04 |
| CHEMBL1475693 | FAMPROFAZONE | 2.0 | 1 | 5.01 |
| CHEMBL1766 | DESOXIMETASONE | 4.0 | 1 | 5.00 |
| CHEMBL517427 | NILVADIPINE | 3.0 | 1 | 4.98 |
| CHEMBL1351761 | DINALINE | -1.0 | 1 | 4.90 |
| CHEMBL2356116 | — | — | 1 | 4.90 |
| CHEMBL1411951 | — | — | 1 | 4.90 |
| CHEMBL1318553 | — | — | 1 | 4.85 |
| CHEMBL1480 | FELODIPINE | 4.0 | 1 | 4.63 |
| CHEMBL13828 | OXATOMIDE | 2.0 | 1 | 4.60 |
| CHEMBL1080983 | FEBANTEL | 2.0 | 1 | 4.50 |
| CHEMBL1726 | NISOLDIPINE | 4.0 | 1 | 4.50 |
| CHEMBL347036 | PROADIFEN HYDROCHLORIDE | -1.0 | 1 | 4.45 |
| CHEMBL1870919 | BUMECAINE | 2.0 | 1 | 4.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL94657 | PATUPILONE | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL312862 | DEMECOLCINE | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL1237054 | PLICAMYCIN | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1200600 | FLUOROMETHOLONE | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL542541 | HYDRALAZINE HYDROCHLORIDE | EC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1200617 | RIMEXOLONE | EC50 | = | 680.0 | nM | 6.17 |
| CHEMBL1891684 | RIODIPINE | EC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL98 | VORINOSTAT | EC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL384467 | DEXAMETHASONE | EC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL474260 | CARUBICIN | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL650 | METHYLPREDNISOLONE | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL37161 | FENBENDAZOLE | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL1530428 | DEXAMETHASONE ACETATE | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL1702784 | — | EC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL52606 | COLFORSIN | EC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL284733 | DICLAZURIL | EC50 | = | 9000.0 | nM | 5.05 |
| CHEMBL1714574 | TERCONAZOLE | EC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL1475693 | FAMPROFAZONE | EC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL1766 | DESOXIMETASONE | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL517427 | NILVADIPINE | EC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL1351761 | DINALINE | EC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL2356116 | — | EC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL1411951 | — | EC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL1318553 | — | EC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL1480 | FELODIPINE | EC50 | = | 23400.0 | nM | 4.63 |
| CHEMBL13828 | OXATOMIDE | EC50 | = | 25100.0 | nM | 4.60 |
| CHEMBL1726 | NISOLDIPINE | EC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL1080983 | FEBANTEL | EC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL347036 | PROADIFEN HYDROCHLORIDE | EC50 | = | 35500.0 | nM | 4.45 |
| CHEMBL1870919 | BUMECAINE | EC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL450613 | ZERANOL | EC50 | = | 38400.0 | nM | 4.42 |
| CHEMBL1201065 | THIAMYLAL SODIUM | EC50 | = | 45900.0 | nM | 4.34 |
| CHEMBL603 | ZAFIRLUKAST | EC50 | = | 58400.0 | nM | 4.23 |
| CHEMBL2103827 | DROXIDOPA | EC50 | = | 63100.0 | nM | 4.20 |
| CHEMBL242080 | E319 | EC50 | - | — | - | |
| CHEMBL1200902 | — | EC50 | - | — | - |