Assay Detail
Binding
CHEMBL676106
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Binding affinity towards Endothelin A receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery, modeling, and human pharmacokinetics of N-(2-acetyl-4,6-dimethylphenyl)-3-(3,4-dimethylisoxazol-5-ylsulfamoyl)thiophene-2-carboxamide (TBC3711), a second generation, ETA selective, and orally bioavailable endothelin antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 9.26 | 10.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9194 | ATRASENTAN | 3.0 | 1 | 10.47 |
| CHEMBL305576 | — | — | 1 | 10.47 |
| CHEMBL282724 | SITAXENTAN | 4.0 | 1 | 9.37 |
| CHEMBL24461 | — | — | 1 | 8.85 |
| CHEMBL23261 | DARUSENTAN | 3.0 | 1 | 8.22 |
| CHEMBL957 | BOSENTAN | 4.0 | 1 | 8.19 |
| CHEMBL314691 | BQ-123 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9194 | ATRASENTAN | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL305576 | — | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL282724 | SITAXENTAN | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL24461 | — | Ki | = | 1.4 | nM | 8.85 |
| CHEMBL23261 | DARUSENTAN | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL957 | BOSENTAN | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL314691 | BQ-123 | Ki | - | nM | - |