Assay Detail
Binding
CHEMBL677273
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Binding affinity against human ETB receptor in transfected COS 7 cell membrane preparation
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | COS 7 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 5.07 | 6.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL76623 | — | — | 1 | 6.85 |
| CHEMBL311258 | — | — | 1 | 6.21 |
| CHEMBL80782 | — | — | 1 | 5.48 |
| CHEMBL267458 | BMS-182874 | — | 1 | 4.85 |
| CHEMBL80980 | — | — | 1 | 4.80 |
| CHEMBL76860 | — | — | 1 | 4.57 |
| CHEMBL77962 | — | — | 1 | 4.34 |
| CHEMBL27065 | — | — | 1 | 4.31 |
| CHEMBL310427 | — | — | 1 | 4.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL76623 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL311258 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL80782 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL267458 | BMS-182874 | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL80980 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL76860 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL77962 | — | IC50 | = | 46000.0 | nM | 4.34 |
| CHEMBL27065 | — | IC50 | = | 49000.0 | nM | 4.31 |
| CHEMBL310427 | — | IC50 | = | 55000.0 | nM | 4.26 |