Assay Detail
Functional
CHEMBL2060170
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human endothelin receptor subtype A expressed in CHO-K1 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and biological evaluation of 4'-[(benzimidazole-1-yl)methyl]biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 7.79 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2058372 | — | — | 1 | 8.05 |
| CHEMBL957 | BOSENTAN | 4.0 | 1 | 8.05 |
| CHEMBL2058371 | — | — | 1 | 8.03 |
| CHEMBL2058373 | — | — | 1 | 8.02 |
| CHEMBL2058370 | — | — | 1 | 8.01 |
| CHEMBL2058374 | — | — | 1 | 8.01 |
| CHEMBL2058375 | — | — | 1 | 8.00 |
| CHEMBL2058376 | — | — | 1 | 8.00 |
| CHEMBL2058377 | — | — | 1 | 7.96 |
| CHEMBL2058369 | — | — | 1 | 7.66 |
| CHEMBL2058368 | — | — | 1 | 7.41 |
| CHEMBL2058367 | — | — | 1 | 7.12 |
| CHEMBL2058366 | — | — | 1 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2058372 | — | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL957 | BOSENTAN | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL2058371 | — | IC50 | = | 9.3 | nM | 8.03 |
| CHEMBL2058373 | — | IC50 | = | 9.6 | nM | 8.02 |
| CHEMBL2058370 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL2058374 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL2058375 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2058376 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2058377 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL2058369 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2058368 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL2058367 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL2058366 | — | IC50 | = | 99.0 | nM | 7.00 |