Assay Detail
ADMET
CHEMBL3531531
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
52
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | HepG2 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Nuclear receptor subfamily 1 group I member 2 (CHEMBL3401) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification of clinically used drugs that activate pregnane X receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 52 | 4.90 | 5.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL517427 | NILVADIPINE | 3.0 | 1 | 5.70 |
| CHEMBL2356116 | — | — | 1 | 5.50 |
| CHEMBL374478 | RIFAMPIN | 4.0 | 1 | 5.46 |
| CHEMBL40883 | — | — | 1 | 5.46 |
| CHEMBL1480 | FELODIPINE | 4.0 | 1 | 5.41 |
| CHEMBL1535402 | — | — | 1 | 5.40 |
| CHEMBL1200617 | RIMEXOLONE | 4.0 | 1 | 5.40 |
| CHEMBL1891684 | RIODIPINE | 2.0 | 1 | 5.40 |
| CHEMBL163 | RITONAVIR | 4.0 | 1 | 5.40 |
| CHEMBL1201065 | THIAMYLAL SODIUM | 4.0 | 1 | 5.39 |
| CHEMBL1475693 | FAMPROFAZONE | 2.0 | 1 | 5.29 |
| CHEMBL13828 | OXATOMIDE | 2.0 | 1 | 5.15 |
| CHEMBL52606 | COLFORSIN | 2.0 | 1 | 5.10 |
| CHEMBL1714574 | TERCONAZOLE | 4.0 | 1 | 5.05 |
| CHEMBL998 | LORATADINE | 4.0 | 1 | 5.00 |
| CHEMBL37161 | FENBENDAZOLE | 2.0 | 1 | 5.00 |
| CHEMBL1726 | NISOLDIPINE | 4.0 | 1 | 5.00 |
| CHEMBL1870919 | BUMECAINE | 2.0 | 1 | 4.96 |
| CHEMBL1702784 | — | — | 1 | 4.95 |
| CHEMBL1200902 | — | — | 1 | 4.90 |
| CHEMBL242080 | E319 | — | 1 | 4.90 |
| CHEMBL1411951 | — | — | 1 | 4.90 |
| CHEMBL312862 | DEMECOLCINE | 2.0 | 1 | 4.90 |
| CHEMBL94657 | PATUPILONE | 3.0 | 1 | 4.90 |
| CHEMBL1200600 | FLUOROMETHOLONE | 4.0 | 1 | 4.90 |
| CHEMBL7002 | CIGLITAZONE | 2.0 | 1 | 4.85 |
| CHEMBL1735 | INDINAVIR SULFATE | 4.0 | 1 | 4.85 |
| CHEMBL1617 | RIFAXIMIN | 4.0 | 1 | 4.85 |
| CHEMBL1318553 | — | — | 1 | 4.85 |
| CHEMBL957 | BOSENTAN | 4.0 | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL517427 | NILVADIPINE | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL2356116 | — | EC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL374478 | RIFAMPIN | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL40883 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL1480 | FELODIPINE | EC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL1535402 | — | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL1200617 | RIMEXOLONE | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL1891684 | RIODIPINE | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL163 | RITONAVIR | EC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL1201065 | THIAMYLAL SODIUM | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL1475693 | FAMPROFAZONE | EC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL13828 | OXATOMIDE | EC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL52606 | COLFORSIN | EC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL1714574 | TERCONAZOLE | EC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL1726 | NISOLDIPINE | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL37161 | FENBENDAZOLE | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL998 | LORATADINE | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1870919 | BUMECAINE | EC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1702784 | — | EC50 | = | 11200.0 | nM | 4.95 |
| CHEMBL1200902 | — | EC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL242080 | E319 | EC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL1411951 | — | EC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL312862 | DEMECOLCINE | EC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL94657 | PATUPILONE | EC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL1200600 | FLUOROMETHOLONE | EC50 | = | 12600.0 | nM | 4.90 |
| CHEMBL7002 | CIGLITAZONE | EC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL603 | ZAFIRLUKAST | EC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL957 | BOSENTAN | EC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL1617 | RIFAXIMIN | EC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL1735 | INDINAVIR SULFATE | EC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL1318553 | — | EC50 | = | 14100.0 | nM | 4.85 |
| CHEMBL1080983 | FEBANTEL | EC50 | = | 15800.0 | nM | 4.80 |
| CHEMBL300555 | SPIROXATRINE | EC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL2361572 | — | EC50 | = | 22400.0 | nM | 4.65 |
| CHEMBL450613 | ZERANOL | EC50 | = | 23700.0 | nM | 4.62 |
| CHEMBL1200807 | NORELGESTROMIN | EC50 | = | 25100.0 | nM | 4.60 |
| CHEMBL2107554 | SODIUM DIBUNATE | EC50 | = | 25100.0 | nM | 4.60 |
| CHEMBL347036 | PROADIFEN HYDROCHLORIDE | EC50 | = | 25100.0 | nM | 4.60 |
| CHEMBL1351761 | DINALINE | EC50 | = | 28200.0 | nM | 4.55 |
| CHEMBL304818 | DOCEBENONE | EC50 | = | 28200.0 | nM | 4.55 |
| CHEMBL1200402 | AMLODIPINE BESYLATE | EC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL2104261 | ENZACAMENE | EC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL1111 | AMBRISENTAN | EC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL3189011 | — | EC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL465 | DRONABINOL | EC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL408 | TROGLITAZONE | EC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL284733 | DICLAZURIL | EC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL596 | FENTANYL | EC50 | = | 31600.0 | nM | 4.50 |
| CHEMBL98 | VORINOSTAT | EC50 | = | 35500.0 | nM | 4.45 |
| CHEMBL1200596 | CHLOROXINE | EC50 | = | 39800.0 | nM | 4.40 |