Assay Detail
Binding
CHEMBL672256
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Receptor binding affinity was determined against [125I]ET1 with membranes prepared from human placenta for ETB receptor
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 7.05 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL437472 | ENDOTHELIN | 2.0 | 1 | 9.70 |
| CHEMBL72037 | — | — | 1 | 8.30 |
| CHEMBL308088 | — | — | 1 | 7.85 |
| CHEMBL70339 | — | — | 1 | 7.72 |
| CHEMBL70385 | — | — | 1 | 7.60 |
| CHEMBL70895 | — | — | 1 | 7.60 |
| CHEMBL70203 | — | — | 1 | 7.37 |
| CHEMBL70293 | — | — | 1 | 7.31 |
| CHEMBL70487 | — | — | 1 | 7.22 |
| CHEMBL303428 | — | — | 1 | 7.20 |
| CHEMBL72473 | — | — | 1 | 7.16 |
| CHEMBL70800 | — | — | 1 | 6.92 |
| CHEMBL303649 | — | — | 1 | 6.84 |
| CHEMBL957 | BOSENTAN | 4.0 | 1 | 6.82 |
| CHEMBL71070 | — | — | 1 | 6.80 |
| CHEMBL70303 | — | — | 1 | 6.77 |
| CHEMBL70365 | — | — | 1 | 6.70 |
| CHEMBL435895 | — | — | 1 | 6.52 |
| CHEMBL70788 | — | — | 1 | 6.16 |
| CHEMBL70781 | — | — | 1 | 6.11 |
| CHEMBL74118 | — | — | 1 | 6.00 |
| CHEMBL70924 | — | — | 1 | 5.91 |
| CHEMBL307803 | — | — | 1 | 5.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL437472 | ENDOTHELIN | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL72037 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL308088 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL70339 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL70385 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL70895 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL70203 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL70293 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL70487 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL303428 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL72473 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL70800 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL303649 | — | IC50 | = | 144.0 | nM | 6.84 |
| CHEMBL957 | BOSENTAN | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL71070 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL70303 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL70365 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL435895 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL70788 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL70781 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL74118 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL70924 | — | IC50 | = | 1240.0 | nM | 5.91 |
| CHEMBL307803 | — | IC50 | = | 2800.0 | nM | 5.55 |