Assay Detail
Functional
CHEMBL975041
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human pregnane X receptor expressed in HGPXR reporter cells
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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
N-1H-benzimidazol-5-ylbenzenesulfonamide derivatives as potent hPXR agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 7.11 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL463678 | — | — | 1 | 9.15 |
| CHEMBL464497 | — | — | 1 | 8.82 |
| CHEMBL465733 | — | — | 1 | 7.89 |
| CHEMBL457270 | — | — | 1 | 7.70 |
| CHEMBL464867 | — | — | 1 | 7.70 |
| CHEMBL513946 | — | — | 1 | 7.64 |
| CHEMBL464496 | — | — | 1 | 7.48 |
| CHEMBL463679 | — | — | 1 | 7.38 |
| CHEMBL517474 | — | — | 1 | 7.35 |
| CHEMBL457271 | — | — | 1 | 7.31 |
| CHEMBL516308 | — | — | 1 | 7.29 |
| CHEMBL517181 | — | — | 1 | 7.28 |
| CHEMBL514896 | — | — | 1 | 7.26 |
| CHEMBL465058 | — | — | 1 | 7.26 |
| CHEMBL516337 | — | — | 1 | 7.00 |
| CHEMBL516149 | — | — | 1 | 6.75 |
| CHEMBL514421 | — | — | 1 | 6.71 |
| CHEMBL464687 | — | — | 1 | 6.66 |
| CHEMBL457277 | — | — | 1 | 6.57 |
| CHEMBL457278 | — | — | 1 | 6.47 |
| CHEMBL457297 | — | — | 1 | 6.47 |
| CHEMBL457296 | — | — | 1 | 6.42 |
| CHEMBL457674 | — | — | 1 | 6.42 |
| CHEMBL458775 | — | — | 1 | 6.41 |
| CHEMBL457272 | — | — | 1 | 6.37 |
| CHEMBL464686 | — | — | 1 | 6.29 |
| CHEMBL457487 | — | — | 1 | 5.84 |
| CHEMBL464866 | — | — | 1 | - |
| CHEMBL518091 | — | — | 1 | - |
| CHEMBL458774 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL463678 | — | EC50 | = | 0.7 | nM | 9.15 |
| CHEMBL464497 | — | EC50 | = | 1.5 | nM | 8.82 |
| CHEMBL465733 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL457270 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL464867 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL513946 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL464496 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL463679 | — | EC50 | = | 42.0 | nM | 7.38 |
| CHEMBL517474 | — | EC50 | = | 45.0 | nM | 7.35 |
| CHEMBL457271 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL516308 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL517181 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL514896 | — | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL465058 | — | EC50 | = | 55.0 | nM | 7.26 |
| CHEMBL516337 | — | EC50 | = | 101.0 | nM | 7.00 |
| CHEMBL516149 | — | EC50 | = | 176.0 | nM | 6.75 |
| CHEMBL514421 | — | EC50 | = | 197.0 | nM | 6.71 |
| CHEMBL464687 | — | EC50 | = | 217.0 | nM | 6.66 |
| CHEMBL457277 | — | EC50 | = | 271.0 | nM | 6.57 |
| CHEMBL457278 | — | EC50 | = | 336.0 | nM | 6.47 |
| CHEMBL457297 | — | EC50 | = | 340.0 | nM | 6.47 |
| CHEMBL457296 | — | EC50 | = | 376.0 | nM | 6.42 |
| CHEMBL457674 | — | EC50 | = | 385.0 | nM | 6.42 |
| CHEMBL458775 | — | EC50 | = | 388.0 | nM | 6.41 |
| CHEMBL457272 | — | EC50 | = | 428.0 | nM | 6.37 |
| CHEMBL464686 | — | EC50 | = | 515.0 | nM | 6.29 |
| CHEMBL457487 | — | EC50 | = | 1456.0 | nM | 5.84 |
| CHEMBL464866 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL518091 | — | EC50 | > | 5000.0 | nM | - |
| CHEMBL458774 | — | EC50 | > | 5000.0 | nM | - |