Assay Detail
Binding
CHEMBL5239751
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BODIPY FL vindoline binding to recombinant human GST-tagged PXR LBD (111 to 434 residues) expressed in baculovirus infected insect cells incubated for 1 mins under shaking condition followed by 60 mins under dark condition by TR-FRET assay
92
Total Activities
92
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 78 | 6.50 | 8.40 |
| Inhibition | 14 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5277255 | — | — | 1 | 8.40 |
| CHEMBL5284539 | — | — | 1 | 8.22 |
| CHEMBL5282848 | — | — | 1 | 8.15 |
| CHEMBL5285451 | — | — | 1 | 8.15 |
| CHEMBL5274748 | — | — | 1 | 7.96 |
| CHEMBL5288280 | — | — | 1 | 7.92 |
| CHEMBL5274800 | — | — | 1 | 7.85 |
| CHEMBL5277006 | — | — | 1 | 7.82 |
| CHEMBL5290100 | — | — | 1 | 7.80 |
| CHEMBL5269977 | — | — | 1 | 7.80 |
| CHEMBL5281952 | — | — | 1 | 7.75 |
| CHEMBL5289969 | — | — | 1 | 7.70 |
| CHEMBL5271698 | — | — | 1 | 7.66 |
| CHEMBL5276468 | — | — | 1 | 7.66 |
| CHEMBL62136 | T091317 | — | 1 | 7.58 |
| CHEMBL5286999 | — | — | 1 | 7.58 |
| CHEMBL5291207 | — | — | 1 | 7.57 |
| CHEMBL5277482 | — | — | 1 | 7.57 |
| CHEMBL5280042 | — | — | 1 | 7.55 |
| CHEMBL5288757 | — | — | 1 | 7.41 |
| CHEMBL5290088 | — | — | 1 | 7.40 |
| CHEMBL5278206 | — | — | 1 | 7.28 |
| CHEMBL5270384 | — | — | 1 | 7.23 |
| CHEMBL5267038 | — | — | 1 | 7.16 |
| CHEMBL5277595 | — | — | 1 | 7.07 |
| CHEMBL5287237 | — | — | 1 | 7.03 |
| CHEMBL5286475 | — | — | 1 | 6.92 |
| CHEMBL5267901 | — | — | 1 | 6.92 |
| CHEMBL5266231 | — | — | 1 | 6.77 |
| CHEMBL5316222 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5277255 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5284539 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5285451 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5282848 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5274748 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5288280 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5274800 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5277006 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5290100 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5269977 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5281952 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5289969 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5271698 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5276468 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5286999 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL62136 | T091317 | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5291207 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5277482 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5280042 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL5288757 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5290088 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5278206 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5270384 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5267038 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5277595 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL5287237 | — | IC50 | = | 93.0 | nM | 7.03 |
| CHEMBL5267901 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5286475 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5266231 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5316222 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5276535 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL5271913 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5287939 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL5269205 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5278057 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5273565 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL5268267 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL5276676 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL5277632 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL5276756 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5289489 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL5290246 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL5269952 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL5287648 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL5266983 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL5273045 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5272707 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL5273985 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL5279641 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL5287193 | — | IC50 | = | 1000.0 | nM | 6.00 |