Assay Detail
Binding
CHEMBL677443
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Binding affinity towards human cloned endothelin B receptor by [125I]ET1 displacement.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
The design and synthesis of a novel series of indole derived selective ET(A) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.46 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL23261 | DARUSENTAN | 3.0 | 1 | 7.80 |
| CHEMBL262784 | — | — | 1 | 7.47 |
| CHEMBL539420 | — | — | 1 | 7.17 |
| CHEMBL280379 | — | — | 1 | 7.03 |
| CHEMBL279703 | — | — | 1 | 6.69 |
| CHEMBL433221 | — | — | 1 | 6.68 |
| CHEMBL276982 | — | — | 1 | 6.64 |
| CHEMBL22562 | — | — | 1 | 6.52 |
| CHEMBL22367 | — | — | 1 | 6.51 |
| CHEMBL22513 | — | — | 1 | 6.40 |
| CHEMBL279947 | — | — | 1 | 6.35 |
| CHEMBL23444 | — | — | 1 | 6.32 |
| CHEMBL278109 | — | — | 1 | 6.11 |
| CHEMBL278349 | — | — | 1 | 6.07 |
| CHEMBL22249 | — | — | 1 | 5.98 |
| CHEMBL433619 | — | — | 1 | 5.96 |
| CHEMBL2114305 | — | — | 1 | 5.82 |
| CHEMBL23833 | — | — | 1 | 5.66 |
| CHEMBL24015 | — | — | 1 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL23261 | DARUSENTAN | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL262784 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL539420 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL280379 | — | IC50 | = | 94.0 | nM | 7.03 |
| CHEMBL279703 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL433221 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL276982 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL22562 | — | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL22367 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL22513 | — | IC50 | = | 397.0 | nM | 6.40 |
| CHEMBL279947 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL23444 | — | IC50 | = | 474.0 | nM | 6.32 |
| CHEMBL278109 | — | IC50 | = | 774.0 | nM | 6.11 |
| CHEMBL278349 | — | IC50 | = | 846.0 | nM | 6.07 |
| CHEMBL22249 | — | IC50 | = | 1056.0 | nM | 5.98 |
| CHEMBL433619 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL2114305 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL23833 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL24015 | — | IC50 | = | 2570.0 | nM | 5.59 |