Assay Detail
Binding
CHEMBL672902
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Binding affinity towards displacement of [125 I] ET-3 from COS-7 cells transfected with porcine Endothelin B receptor
18
Total Activities
18
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
Discovery and synthesis of a potent sulfonamide ET(B) selective antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.41 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54057 | — | — | 1 | 8.70 |
| CHEMBL54998 | — | — | 1 | 7.70 |
| CHEMBL54703 | — | — | 1 | 7.07 |
| CHEMBL55909 | — | — | 1 | 6.85 |
| CHEMBL298395 | — | — | 1 | 6.62 |
| CHEMBL54770 | — | — | 1 | 6.62 |
| CHEMBL59425 | — | — | 1 | 6.52 |
| CHEMBL298340 | — | — | 1 | 6.51 |
| CHEMBL54274 | — | — | 1 | 6.40 |
| CHEMBL53168 | — | — | 1 | 6.37 |
| CHEMBL54773 | — | — | 1 | 6.30 |
| CHEMBL53097 | — | — | 1 | 6.30 |
| CHEMBL300066 | — | — | 1 | 6.28 |
| CHEMBL55876 | — | — | 1 | 6.25 |
| CHEMBL55664 | — | — | 1 | 5.55 |
| CHEMBL415942 | — | — | 1 | 4.52 |
| CHEMBL417595 | — | — | 1 | 4.46 |
| CHEMBL298976 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54057 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL54998 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL54703 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL55909 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL298395 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL54770 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL59425 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL298340 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL54274 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL53168 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL54773 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL53097 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL300066 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL55876 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL55664 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL415942 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL417595 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL298976 | — | IC50 | > | 1000000.0 | nM | - |