Assay Detail
Binding
CHEMBL5239753
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human PXR in human HepG2 cells co-expressing luciferase gene under control of CYP3A4 promoter assessed as transcriptional activation incubated for 24 hrs by luminescence based analysis
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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
Design and Optimization of 1<i>H</i>-1,2,3-Triazole-4-carboxamides as Novel, Potent, and Selective Inverse Agonists and Antagonists of PXR.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 25 | 5.91 | 8.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5274748 | — | — | 1 | 8.09 |
| CHEMBL5268267 | — | — | 1 | 6.82 |
| CHEMBL5287237 | — | — | 1 | 6.62 |
| CHEMBL5273515 | — | — | 1 | 6.55 |
| CHEMBL5279641 | — | — | 1 | 6.52 |
| CHEMBL5280042 | — | — | 1 | 6.32 |
| CHEMBL5276756 | — | — | 1 | 6.24 |
| CHEMBL5280444 | — | — | 1 | 6.13 |
| CHEMBL5269184 | — | — | 1 | 6.05 |
| CHEMBL5285078 | — | — | 1 | 6.00 |
| CHEMBL5278057 | — | — | 1 | 6.00 |
| CHEMBL374478 | RIFAMPIN | 4.0 | 1 | 5.93 |
| CHEMBL5278206 | — | — | 1 | 5.83 |
| CHEMBL5286475 | — | — | 1 | 5.78 |
| CHEMBL5275510 | — | — | 1 | 5.70 |
| CHEMBL5267901 | — | — | 1 | 5.62 |
| CHEMBL5270149 | — | — | 1 | 5.55 |
| CHEMBL5271191 | — | — | 1 | 5.46 |
| CHEMBL5290246 | — | — | 1 | 5.43 |
| CHEMBL5276676 | — | — | 1 | 5.39 |
| CHEMBL5271121 | — | — | 1 | 5.37 |
| CHEMBL5283855 | — | — | 1 | 5.36 |
| CHEMBL5287498 | — | — | 1 | 5.34 |
| CHEMBL5276093 | — | — | 1 | 4.99 |
| CHEMBL5277556 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5274748 | — | EC50 | = | 8.1 | nM | 8.09 |
| CHEMBL5268267 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5287237 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5273515 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5279641 | — | EC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5280042 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL5276756 | — | EC50 | = | 570.0 | nM | 6.24 |
| CHEMBL5280444 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL5269184 | — | EC50 | = | 900.0 | nM | 6.05 |
| CHEMBL5285078 | — | EC50 | = | 990.0 | nM | 6.00 |
| CHEMBL5278057 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL374478 | RIFAMPIN | EC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL5278206 | — | EC50 | = | 1480.0 | nM | 5.83 |
| CHEMBL5286475 | — | EC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL5275510 | — | EC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5267901 | — | EC50 | = | 2410.0 | nM | 5.62 |
| CHEMBL5270149 | — | EC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL5271191 | — | EC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL5290246 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL5276676 | — | EC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL5271121 | — | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL5283855 | — | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL5287498 | — | EC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL5276093 | — | EC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL5277556 | — | EC50 | = | 25000.0 | nM | 4.60 |