Assay Detail
Binding
CHEMBL682974
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Receptor binding affinity was determined against [125I]ET1 with recombinant human ETA receptor, expressed in baculovirus-infected Sf9 cells
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | Sf9 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Discovery of Ro 48-5695: A potent mixed endothelin receptor antagonist optimized from bosentan
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.68 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL70385 | — | — | 1 | 9.70 |
| CHEMBL437472 | ENDOTHELIN | 2.0 | 1 | 9.70 |
| CHEMBL72037 | — | — | 1 | 9.52 |
| CHEMBL308088 | — | — | 1 | 9.00 |
| CHEMBL70895 | — | — | 1 | 8.52 |
| CHEMBL70293 | — | — | 1 | 8.40 |
| CHEMBL70303 | — | — | 1 | 8.40 |
| CHEMBL70203 | — | — | 1 | 8.22 |
| CHEMBL70800 | — | — | 1 | 8.22 |
| CHEMBL70487 | — | — | 1 | 8.15 |
| CHEMBL71070 | — | — | 1 | 8.15 |
| CHEMBL303428 | — | — | 1 | 8.05 |
| CHEMBL303649 | — | — | 1 | 7.85 |
| CHEMBL70339 | — | — | 1 | 7.77 |
| CHEMBL70365 | — | — | 1 | 7.52 |
| CHEMBL70924 | — | — | 1 | 7.10 |
| CHEMBL957 | BOSENTAN | 4.0 | 1 | 7.10 |
| CHEMBL70781 | — | — | 1 | 6.06 |
| CHEMBL70788 | — | — | 1 | 6.05 |
| CHEMBL74118 | — | — | 1 | 5.96 |
| CHEMBL72473 | — | — | 1 | 5.82 |
| CHEMBL435895 | — | — | 1 | 5.77 |
| CHEMBL307803 | — | — | 1 | 5.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL70385 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL437472 | ENDOTHELIN | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL72037 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL308088 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL70895 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL70293 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL70303 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL70203 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL70800 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL70487 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL71070 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL303428 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL303649 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL70339 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL70365 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL70924 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL957 | BOSENTAN | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL70781 | — | IC50 | = | 880.0 | nM | 6.06 |
| CHEMBL70788 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL74118 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL72473 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL435895 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL307803 | — | IC50 | = | 1900.0 | nM | 5.72 |