Assay Detail
Functional
CHEMBL677406
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of ET-1 stimulated arachidonic acid release in CHO cells expressing rat ET- B receptors
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of the potent combined endothelin-A/endothelin-B receptor antagonist Ac-DDip16-Leu-Asp-Ile-Ile-Trp21: development of endothelin-B receptor selective antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 13 | 6.08 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL328942 | — | — | 1 | 7.70 |
| CHEMBL433406 | — | — | 1 | 7.70 |
| CHEMBL323331 | — | — | 1 | 6.66 |
| CHEMBL384052 | — | — | 1 | 6.54 |
| CHEMBL386181 | — | — | 1 | 6.54 |
| CHEMBL414082 | — | — | 1 | 6.25 |
| CHEMBL262229 | — | — | 1 | 6.05 |
| CHEMBL265734 | — | — | 1 | 5.60 |
| CHEMBL264579 | — | — | 1 | 5.44 |
| CHEMBL413179 | — | — | 1 | 5.40 |
| CHEMBL319537 | — | — | 1 | 5.04 |
| CHEMBL415238 | — | — | 1 | 5.03 |
| CHEMBL407933 | — | — | 1 | 5.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL328942 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL433406 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL323331 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL384052 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL386181 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL414082 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL262229 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL265734 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL264579 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL413179 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL319537 | — | IC50 | = | 9200.0 | nM | 5.04 |
| CHEMBL415238 | — | IC50 | = | 9300.0 | nM | 5.03 |
| CHEMBL407933 | — | IC50 | = | 9300.0 | nM | 5.03 |