Assay Detail
Binding
CHEMBL679704
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In vitro inhibition of [125 I]ET-1 binding to Endothelin A receptor in porcine aortic membrane.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Modifications and structure-activity relationships at the 2-position of 4-sulfonamidopyrimidine derivatives as potent endothelin antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 9.15 | 10.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL170908 | — | — | 1 | 10.59 |
| CHEMBL170493 | — | — | 1 | 10.37 |
| CHEMBL167314 | — | — | 1 | 9.82 |
| CHEMBL168604 | — | — | 1 | 9.70 |
| CHEMBL354528 | — | — | 1 | 9.35 |
| CHEMBL424358 | — | — | 1 | 8.96 |
| CHEMBL168904 | — | — | 1 | 8.80 |
| CHEMBL166875 | — | — | 1 | 8.57 |
| CHEMBL136871 | — | — | 1 | 8.41 |
| CHEMBL957 | BOSENTAN | 4.0 | 1 | 8.12 |
| CHEMBL352775 | — | — | 1 | 8.00 |
| CHEMBL112531 | — | — | 1 | - |
| CHEMBL169872 | — | — | 1 | - |
| CHEMBL112144 | — | — | 1 | - |
| CHEMBL170663 | — | — | 1 | - |
| CHEMBL169667 | — | — | 1 | - |
| CHEMBL354942 | — | — | 1 | - |
| CHEMBL166490 | — | — | 1 | - |
| CHEMBL352479 | — | — | 1 | - |
| CHEMBL352355 | — | — | 1 | - |
| CHEMBL168441 | — | — | 1 | - |
| CHEMBL168119 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL170908 | — | IC50 | = | 0.026 | nM | 10.59 |
| CHEMBL170493 | — | IC50 | = | 0.043 | nM | 10.37 |
| CHEMBL167314 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL168604 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL354528 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL424358 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL168904 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL166875 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL136871 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL957 | BOSENTAN | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL352775 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL112531 | — | IC50 | < | 0.001 | nM | - |
| CHEMBL169872 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL112144 | — | IC50 | = | 0.0039 | nM | - |
| CHEMBL170663 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL169667 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL354942 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL166490 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL352479 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL352355 | — | IC50 | > | 10.0 | nM | - |
| CHEMBL168441 | — | IC50 | = | 0.0053 | nM | - |
| CHEMBL168119 | — | IC50 | = | 0.0025 | nM | - |