Assay Detail
Functional
CHEMBL772606
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Functional vascular ET-1 antagonism was determined in rabbit aorta rings with intact endothelium
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Tissue | Aorta |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 6 | 8.50 | 9.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8823 | SB-209670 | — | 1 | 9.80 |
| CHEMBL302564 | — | — | 1 | 9.24 |
| CHEMBL305980 | — | — | 1 | 9.03 |
| CHEMBL25344 | — | — | 1 | 7.34 |
| CHEMBL267458 | BMS-182874 | — | 1 | 7.09 |
| CHEMBL115951 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8823 | SB-209670 | Kd | = | 0.1585 | nM | 9.80 |
| CHEMBL302564 | — | Kd | = | 0.5754 | nM | 9.24 |
| CHEMBL305980 | — | Kd | = | 0.9333 | nM | 9.03 |
| CHEMBL25344 | — | Kd | = | 45.71 | nM | 7.34 |
| CHEMBL267458 | BMS-182874 | Kd | = | 81.28 | nM | 7.09 |
| CHEMBL115951 | — | Kd | > | 1000.0 | nM | - |