Assay Detail
Binding
CHEMBL5239757
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human PXR in human HepG2 cells co-expressing luciferase gene under control of CYP3A4 promoter assessed as inhibition in rifampicin-induced receptor activation incubated for 24 hrs by luminescence based analysis
60
Total Activities
60
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 |
|---|---|---|---|
| IC50 | 60 | 6.20 | 8.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5281952 | — | — | 1 | 8.16 |
| CHEMBL5277255 | — | — | 1 | 8.05 |
| CHEMBL5286515 | — | — | 1 | 7.85 |
| CHEMBL5284539 | — | — | 1 | 7.85 |
| CHEMBL5289969 | — | — | 1 | 7.82 |
| CHEMBL5285451 | — | — | 1 | 7.75 |
| CHEMBL5274800 | — | — | 1 | 7.13 |
| CHEMBL5290088 | — | — | 1 | 7.03 |
| CHEMBL5282848 | — | — | 1 | 6.96 |
| CHEMBL5269977 | — | — | 1 | 6.92 |
| CHEMBL5284102 | — | — | 1 | 6.92 |
| CHEMBL5277006 | — | — | 1 | 6.92 |
| CHEMBL5277632 | — | — | 1 | 6.89 |
| CHEMBL5276535 | — | — | 1 | 6.82 |
| CHEMBL5286999 | — | — | 1 | 6.82 |
| CHEMBL5288757 | — | — | 1 | 6.68 |
| CHEMBL5266983 | — | — | 1 | 6.68 |
| CHEMBL5316222 | — | — | 1 | 6.64 |
| CHEMBL5277482 | — | — | 1 | 6.62 |
| CHEMBL5276468 | — | — | 1 | 6.62 |
| CHEMBL5288280 | — | — | 1 | 6.60 |
| CHEMBL5291207 | — | — | 1 | 6.55 |
| CHEMBL5271698 | — | — | 1 | 6.52 |
| CHEMBL5287939 | — | — | 1 | 6.47 |
| CHEMBL5280042 | — | — | 1 | 6.40 |
| CHEMBL5273565 | — | — | 1 | 6.39 |
| CHEMBL5286721 | — | — | 1 | 6.36 |
| CHEMBL5267038 | — | — | 1 | 6.34 |
| CHEMBL5266231 | — | — | 1 | 6.34 |
| CHEMBL5271913 | — | — | 1 | 6.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5281952 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL5277255 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5284539 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5286515 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5289969 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5285451 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5274800 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL5290088 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL5282848 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5269977 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5284102 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5277006 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5277632 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5286999 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5276535 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5288757 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5266983 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5316222 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5277482 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5276468 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5288280 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL5291207 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5271698 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL5287939 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5280042 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL5273565 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL5286721 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5267038 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL5266231 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL5271913 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5272707 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL5289489 | — | IC50 | = | 620.0 | nM | 6.21 |
| CHEMBL5277595 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL5270384 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL5274748 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL5266755 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL5289648 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL5287237 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL5279796 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL5269205 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5287048 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5279980 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5274653 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5287648 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5274837 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL5288604 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL5273985 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL5273045 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL5269952 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL5287193 | — | IC50 | = | 4800.0 | nM | 5.32 |