Assay Detail
Binding
CHEMBL681520
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Inhibition of Human Endothelin A receptor expressed in CHO Cells.
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.07 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL29422 | — | — | 1 | 9.70 |
| CHEMBL104848 | — | — | 1 | 9.30 |
| CHEMBL24461 | — | — | 1 | 8.85 |
| CHEMBL104223 | — | — | 1 | 8.70 |
| CHEMBL107574 | — | — | 1 | 8.43 |
| CHEMBL104172 | — | — | 1 | 8.33 |
| CHEMBL106684 | — | — | 1 | 8.33 |
| CHEMBL322674 | — | — | 1 | 7.96 |
| CHEMBL106749 | — | — | 1 | 7.80 |
| CHEMBL105490 | — | — | 1 | 7.75 |
| CHEMBL319924 | — | — | 1 | 7.72 |
| CHEMBL267458 | BMS-182874 | — | 1 | 7.26 |
| CHEMBL106846 | — | — | 1 | 7.16 |
| CHEMBL319036 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL29422 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL104848 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL24461 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL104223 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL107574 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL104172 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL106684 | — | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL322674 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL106749 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL105490 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL319924 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL267458 | BMS-182874 | Ki | = | 55.0 | nM | 7.26 |
| CHEMBL106846 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL319036 | — | Ki | = | 2000.0 | nM | 5.70 |