Assay Detail
Binding
CHEMBL5239755
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at human PXR in human HepG2 cells co-expressing luciferase gene under control of CYP3A4 promoter assessed as inhibition of receptor basal activity incubated for 24 hrs by luminescence based analysis
40
Total Activities
40
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 | 40 | 6.67 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5284539 | — | — | 1 | 9.00 |
| CHEMBL5286515 | — | — | 1 | 8.80 |
| CHEMBL5290088 | — | — | 1 | 8.16 |
| CHEMBL5282848 | — | — | 1 | 7.89 |
| CHEMBL5284102 | — | — | 1 | 7.85 |
| CHEMBL5286999 | — | — | 1 | 7.85 |
| CHEMBL5316222 | — | — | 1 | 7.66 |
| CHEMBL5276468 | — | — | 1 | 7.62 |
| CHEMBL5277632 | — | — | 1 | 7.41 |
| CHEMBL5288280 | — | — | 1 | 7.38 |
| CHEMBL5288757 | — | — | 1 | 7.37 |
| CHEMBL5277482 | — | — | 1 | 7.36 |
| CHEMBL5276535 | — | — | 1 | 7.31 |
| CHEMBL5266983 | — | — | 1 | 7.27 |
| CHEMBL5291207 | — | — | 1 | 7.26 |
| CHEMBL5266231 | — | — | 1 | 7.11 |
| CHEMBL5287939 | — | — | 1 | 6.96 |
| CHEMBL5271913 | — | — | 1 | 6.92 |
| CHEMBL5272707 | — | — | 1 | 6.92 |
| CHEMBL5273565 | — | — | 1 | 6.92 |
| CHEMBL5277595 | — | — | 1 | 6.85 |
| CHEMBL5289489 | — | — | 1 | 6.82 |
| CHEMBL5266755 | — | — | 1 | 6.68 |
| CHEMBL5279796 | — | — | 1 | 6.48 |
| CHEMBL5287048 | — | — | 1 | 6.47 |
| CHEMBL5274653 | — | — | 1 | 6.47 |
| CHEMBL5287648 | — | — | 1 | 6.36 |
| CHEMBL5273045 | — | — | 1 | 6.32 |
| CHEMBL5269952 | — | — | 1 | 5.85 |
| CHEMBL5269205 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5284539 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5286515 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5290088 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL5282848 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5284102 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5286999 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5316222 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5276468 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5277632 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5288280 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5288757 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5277482 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL5276535 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5266983 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL5291207 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5266231 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL5287939 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5271913 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5272707 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5273565 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5277595 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5289489 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5266755 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5279796 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5287048 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5274653 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL5287648 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5273045 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL5269952 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5269205 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5288604 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL5287193 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5276751 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL5267285 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL5274837 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL5276688 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL5286479 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL5268870 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL5277096 | — | IC50 | = | 21500.0 | nM | 4.67 |
| CHEMBL5275863 | — | IC50 | = | 26000.0 | nM | 4.58 |