Assay Detail
Binding
CHEMBL679795
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Inhibition of ET-1 binding to Endothelin A receptor in cultured rabbit renal artery vascular smooth muscle cells
10
Total Activities
10
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 a functional hexapeptide antagonist of endothelin.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.59 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL437472 | ENDOTHELIN | 2.0 | 1 | 9.70 |
| CHEMBL328942 | — | — | 1 | 7.82 |
| CHEMBL317064 | — | — | 1 | 6.89 |
| CHEMBL85341 | — | — | 1 | 6.40 |
| CHEMBL315047 | — | — | 1 | 6.00 |
| CHEMBL86814 | — | — | 1 | 5.55 |
| CHEMBL438194 | — | — | 1 | 5.36 |
| CHEMBL289687 | — | — | 1 | 5.02 |
| CHEMBL432091 | — | — | 1 | - |
| CHEMBL34540 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL437472 | ENDOTHELIN | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL328942 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL317064 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL85341 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL315047 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL86814 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL438194 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL289687 | — | IC50 | = | 9500.0 | nM | 5.02 |
| CHEMBL432091 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL34540 | — | IC50 | > | 50000.0 | nM | - |