Assay Detail
Binding
CHEMBL677445
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity measured in CHO cells stably transfected with the human endothelin B receptor
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 10 | 6.09 | 7.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL421190 | — | — | 1 | 7.43 |
| CHEMBL262993 | — | — | 1 | 6.68 |
| CHEMBL405599 | — | — | 1 | 6.23 |
| CHEMBL265116 | — | — | 1 | 6.05 |
| CHEMBL328942 | — | — | 1 | 6.02 |
| CHEMBL433349 | — | — | 1 | 5.75 |
| CHEMBL384052 | — | — | 1 | 5.36 |
| CHEMBL264579 | — | — | 1 | 5.23 |
| CHEMBL216082 | — | — | 1 | - |
| CHEMBL2370255 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL421190 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL262993 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL405599 | — | IC50 | = | 590.0 | nM | 6.23 |
| CHEMBL265116 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL328942 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL433349 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL384052 | — | IC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL264579 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL216082 | — | IC50 | > | 1600.0 | nM | - |
| CHEMBL2370255 | — | IC50 | > | 10000.0 | nM | - |