Assay Detail
Binding
CHEMBL677265
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Tested for the competitive binding versus [125I]- ET-1 determined in bovine cerebrum membrane for Endothelin B receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Tissue | Cerebrum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Endothelin-1 analogues substituted at both position 18 and 19: highly potent endothelin antagonists with no selectivity for either receptor subtype ETA or ETB.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 9.66 | 10.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL438733 | — | — | 1 | 10.03 |
| CHEMBL437472 | ENDOTHELIN | 2.0 | 1 | 9.92 |
| CHEMBL427748 | — | — | 1 | 9.77 |
| CHEMBL1790962 | — | — | 1 | 9.77 |
| CHEMBL2373292 | — | — | 1 | 9.60 |
| CHEMBL1790963 | — | — | 1 | 9.48 |
| CHEMBL2373291 | — | — | 1 | 9.38 |
| CHEMBL411171 | — | — | 1 | 9.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL438733 | — | IC50 | = | 0.093 | nM | 10.03 |
| CHEMBL437472 | ENDOTHELIN | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL427748 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL1790962 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL2373292 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL1790963 | — | IC50 | = | 0.33 | nM | 9.48 |
| CHEMBL2373291 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL411171 | — | IC50 | = | 0.45 | nM | 9.35 |