Assay Detail
ADMET
CHEMBL3531530
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activation of PXR in human cryopreserved hepatocytes assessed as induction of CYP3A4
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Cell Type | Hepatocyte |
| 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 | 6 | 6.10 | 6.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL13828 | OXATOMIDE | 2.0 | 1 | 6.40 |
| CHEMBL1200617 | RIMEXOLONE | 4.0 | 1 | 6.40 |
| CHEMBL52606 | COLFORSIN | 2.0 | 1 | 6.16 |
| CHEMBL1870919 | BUMECAINE | 2.0 | 1 | 5.96 |
| CHEMBL1475693 | FAMPROFAZONE | 2.0 | 1 | 5.85 |
| CHEMBL517427 | NILVADIPINE | 3.0 | 1 | 5.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL13828 | OXATOMIDE | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1200617 | RIMEXOLONE | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL52606 | COLFORSIN | EC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1870919 | BUMECAINE | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1475693 | FAMPROFAZONE | EC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL517427 | NILVADIPINE | EC50 | = | 1400.0 | nM | 5.85 |