Assay Detail
Binding
CHEMBL679797
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of Endothelin A receptor mediated (ET-1) release of arachidonic acid from rabbit renal artery vascular smooth muscle cells
9
Total Activities
9
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 relationships in a series of orally active gamma-hydroxy butenolide endothelin antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.28 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10862 | — | — | 1 | 9.47 |
| CHEMBL10847 | — | — | 1 | 9.11 |
| CHEMBL10922 | — | — | 1 | 9.01 |
| CHEMBL10832 | — | — | 1 | 8.96 |
| CHEMBL8981 | PD-156707 | — | 1 | 8.96 |
| CHEMBL10905 | — | — | 1 | 8.31 |
| CHEMBL273660 | — | — | 1 | 8.00 |
| CHEMBL10801 | — | — | 1 | 7.31 |
| CHEMBL267094 | — | — | 1 | 5.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10862 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL10847 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL10922 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL10832 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL8981 | PD-156707 | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL10905 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL273660 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL10801 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL267094 | — | IC50 | = | 3800.0 | nM | 5.42 |