Assay Detail
Binding
CHEMBL678557
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards human Endothelin A receptor by measuring its ability to displace [125I]ET1 from CHO cells
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.77 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL303631 | — | — | 1 | 9.92 |
| CHEMBL302564 | — | — | 1 | 9.40 |
| CHEMBL305270 | — | — | 1 | 9.15 |
| CHEMBL305980 | — | — | 1 | 9.05 |
| CHEMBL302753 | — | — | 1 | 9.00 |
| CHEMBL418326 | — | — | 1 | 9.00 |
| CHEMBL25344 | — | — | 1 | 8.22 |
| CHEMBL304778 | — | — | 1 | 8.15 |
| CHEMBL67536 | — | — | 1 | 7.96 |
| CHEMBL306218 | — | — | 1 | 7.72 |
| CHEMBL67084 | — | — | 1 | 7.72 |
| CHEMBL303390 | — | — | 1 | 7.66 |
| CHEMBL65833 | — | — | 1 | 7.62 |
| CHEMBL304721 | — | — | 1 | 7.48 |
| CHEMBL66402 | — | — | 1 | 7.07 |
| CHEMBL63648 | — | — | 1 | 6.89 |
| CHEMBL303501 | — | — | 1 | 6.82 |
| CHEMBL67957 | — | — | 1 | 6.80 |
| CHEMBL66893 | — | — | 1 | 6.76 |
| CHEMBL303034 | — | — | 1 | 6.70 |
| CHEMBL64009 | — | — | 1 | 6.61 |
| CHEMBL67325 | — | — | 1 | 6.60 |
| CHEMBL304173 | — | — | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL303631 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL302564 | — | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL305270 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL305980 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL302753 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL418326 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL25344 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL304778 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL67536 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL306218 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL67084 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL303390 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL65833 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL304721 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL66402 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL63648 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL303501 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL67957 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL66893 | — | Ki | = | 174.0 | nM | 6.76 |
| CHEMBL303034 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL64009 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL67325 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL304173 | — | Ki | = | 340.0 | nM | 6.47 |