Assay Detail
Binding
CHEMBL682108
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Displacement of [125I]-labeled ET-1 from human cloned endothelin A (ETA) receptor
24
Total Activities
24
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 | 24 | 7.99 | 9.26 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22513 | — | — | 1 | 9.26 |
| CHEMBL23261 | DARUSENTAN | 3.0 | 1 | 9.10 |
| CHEMBL22562 | — | — | 1 | 8.96 |
| CHEMBL278109 | — | — | 1 | 8.74 |
| CHEMBL262784 | — | — | 1 | 8.64 |
| CHEMBL280379 | — | — | 1 | 8.55 |
| CHEMBL278349 | — | — | 1 | 8.51 |
| CHEMBL539420 | — | — | 1 | 8.46 |
| CHEMBL22367 | — | — | 1 | 8.30 |
| CHEMBL22249 | — | — | 1 | 8.28 |
| CHEMBL276982 | — | — | 1 | 8.19 |
| CHEMBL433619 | — | — | 1 | 8.12 |
| CHEMBL24015 | — | — | 1 | 7.92 |
| CHEMBL279947 | — | — | 1 | 7.72 |
| CHEMBL2114305 | — | — | 1 | 7.66 |
| CHEMBL433221 | — | — | 1 | 7.52 |
| CHEMBL23752 | — | — | 1 | 7.51 |
| CHEMBL23833 | — | — | 1 | 7.50 |
| CHEMBL281378 | — | — | 1 | 7.46 |
| CHEMBL279703 | — | — | 1 | 7.42 |
| CHEMBL274758 | — | — | 1 | 7.21 |
| CHEMBL23444 | — | — | 1 | 7.14 |
| CHEMBL281121 | — | — | 1 | 7.00 |
| CHEMBL23418 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22513 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL23261 | DARUSENTAN | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL22562 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL278109 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL262784 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL280379 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL278349 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL539420 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL22367 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL22249 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL276982 | — | IC50 | = | 6.5 | nM | 8.19 |
| CHEMBL433619 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL24015 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL279947 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL2114305 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL433221 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL23752 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL23833 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL281378 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL279703 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL274758 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL23444 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL281121 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL23418 | — | IC50 | = | 210.0 | nM | 6.68 |