Assay Detail
Binding
CHEMBL679794
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Displacement of [125I]-ET-1 from Endothelin A receptor of rabbit renal artery vascular smooth muscle cells
14
Total Activities
13
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
Design of C-terminal peptide antagonists of endothelin: structure-activity relationships of ET-[1621, D-His16]
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.64 | 6.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL313984 | — | — | 1 | 6.70 |
| CHEMBL147908 | — | — | 1 | 6.19 |
| CHEMBL2370070 | — | — | 1 | 6.12 |
| CHEMBL146155 | — | — | 1 | 6.03 |
| CHEMBL327350 | — | — | 1 | 5.93 |
| CHEMBL86814 | — | — | 2 | 5.55 |
| CHEMBL330489 | — | — | 1 | 5.10 |
| CHEMBL315658 | — | — | 1 | 5.04 |
| CHEMBL289687 | — | — | 1 | 5.02 |
| CHEMBL273391 | — | — | 1 | 4.74 |
| CHEMBL87724 | — | — | 1 | - |
| CHEMBL312916 | — | — | 1 | - |
| CHEMBL432091 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL313984 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL147908 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL2370070 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL146155 | — | IC50 | = | 930.0 | nM | 6.03 |
| CHEMBL327350 | — | IC50 | = | 1180.0 | nM | 5.93 |
| CHEMBL86814 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL330489 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL315658 | — | IC50 | = | 9100.0 | nM | 5.04 |
| CHEMBL289687 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL273391 | — | IC50 | = | 18400.0 | nM | 4.74 |
| CHEMBL87724 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL312916 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL86814 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL432091 | — | IC50 | > | 50000.0 | nM | - |