Assay Detail
Binding
CHEMBL679117
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro inhibition of [125I]ET1 binding to Endothelin A receptor in porcine aortic membrane from endothelial cells
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Endothelial cell |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Potent and selective ET-A antagonists. 1. Syntheses and structure-activity relationships of N-(6-(2-(aryloxy)ethoxy)-4-pyrimidinyl)sulfonamide derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 9.68 | 10.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL369489 | — | — | 1 | 10.41 |
| CHEMBL176272 | — | — | 1 | 10.10 |
| CHEMBL367445 | — | — | 1 | 9.60 |
| CHEMBL177979 | — | — | 1 | 9.38 |
| CHEMBL175501 | — | — | 1 | 9.32 |
| CHEMBL368796 | — | — | 1 | 9.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL369489 | — | IC50 | = | 0.039 | nM | 10.41 |
| CHEMBL176272 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL367445 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL177979 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL175501 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL368796 | — | IC50 | = | 0.56 | nM | 9.25 |