Assay Detail
Binding
CHEMBL679798
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Inhibition of [125I]endothelin-1 [ET-1] binding to endothelin A receptor (ETA) of rabbit renal artery vascular smooth muscle cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Structure-activity and biophysical studies of the C-terminal hexapeptide of endothelin
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.70 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1791271 | — | — | 1 | 7.85 |
| CHEMBL2369709 | — | — | 1 | 7.40 |
| CHEMBL1791279 | — | — | 1 | 5.75 |
| CHEMBL2369713 | — | — | 1 | 5.50 |
| CHEMBL289687 | — | — | 1 | 5.05 |
| CHEMBL1791280 | — | — | 1 | 4.89 |
| CHEMBL2369710 | — | — | 1 | 4.62 |
| CHEMBL1791272 | — | — | 1 | 4.52 |
| CHEMBL2369711 | — | — | 1 | - |
| CHEMBL34540 | — | — | 1 | - |
| CHEMBL432091 | — | — | 1 | - |
| CHEMBL1791277 | — | — | 1 | - |
| CHEMBL2369714 | — | — | 1 | - |
| CHEMBL2369712 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1791271 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL2369709 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL1791279 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL2369713 | — | IC50 | = | 3200.0 | nM | 5.50 |
| CHEMBL289687 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL1791280 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL2369710 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL1791272 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL2369711 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL34540 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL432091 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL1791277 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL2369714 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL2369712 | — | IC50 | > | 50000.0 | nM | - |