Assay Detail
Functional
CHEMBL891767
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human PXR by transient transfection assay
24
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Target
Nuclear receptor subfamily 1 group I member 2 (CHEMBL3401) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Crystal structure of the PXR-T1317 complex provides a scaffold to examine the potential for receptor antagonism.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Activity | 12 | - | - |
| EC50 | 12 | 6.60 | 8.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL396952 | — | — | 2 | 8.50 |
| CHEMBL430006 | — | — | 2 | 8.00 |
| CHEMBL62136 | T091317 | — | 2 | 7.90 |
| CHEMBL242293 | — | — | 2 | 7.80 |
| CHEMBL388024 | — | — | 2 | 6.90 |
| CHEMBL242528 | — | — | 2 | 6.80 |
| CHEMBL242527 | — | — | 2 | 6.30 |
| CHEMBL242526 | — | — | 2 | 6.00 |
| CHEMBL396953 | — | — | 2 | 6.00 |
| CHEMBL242291 | — | — | 2 | 5.00 |
| CHEMBL396041 | — | — | 2 | 5.00 |
| CHEMBL389979 | — | — | 2 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL396952 | — | EC50 | = | 3.162 | nM | 8.50 |
| CHEMBL430006 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL62136 | T091317 | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL242293 | — | EC50 | = | 15.85 | nM | 7.80 |
| CHEMBL388024 | — | EC50 | = | 125.89 | nM | 6.90 |
| CHEMBL242528 | — | EC50 | = | 158.49 | nM | 6.80 |
| CHEMBL242527 | — | EC50 | = | 501.19 | nM | 6.30 |
| CHEMBL242526 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL396953 | — | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL242291 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL396041 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL389979 | — | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL242527 | — | Activity | = | 104.0 | % | - |
| CHEMBL242526 | — | Activity | = | 90.0 | % | - |
| CHEMBL242293 | — | Activity | = | 99.0 | % | - |
| CHEMBL396952 | — | Activity | = | 103.0 | % | - |
| CHEMBL388024 | — | Activity | = | 101.0 | % | - |
| CHEMBL396041 | — | Activity | = | 45.0 | % | - |
| CHEMBL389979 | — | Activity | = | 23.0 | % | - |
| CHEMBL396953 | — | Activity | = | 139.0 | % | - |
| CHEMBL62136 | T091317 | Activity | = | 93.0 | % | - |
| CHEMBL430006 | — | Activity | = | 98.0 | % | - |
| CHEMBL242528 | — | Activity | = | 96.0 | % | - |
| CHEMBL242291 | — | Activity | = | 11.0 | % | - |