Assay Detail
Binding
CHEMBL677447
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Binding affinity towards Endothelin B receptor in human girardi heart cell membranes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Heart |
| Cell Type | heart |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Synthesis and structure-activity relationships of 2-substituted D-tryptophan-containing peptidic endothelin receptor antagonists: importance of the C-2 substituent of the D-tryptophan residue for endothelin A and B receptor subtype selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 7.94 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL73925 | — | — | 1 | 8.96 |
| CHEMBL307936 | — | — | 1 | 8.40 |
| CHEMBL306123 | — | — | 1 | 8.30 |
| CHEMBL2304017 | — | — | 1 | 7.54 |
| CHEMBL2304006 | — | — | 1 | 7.54 |
| CHEMBL2304015 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL73925 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL307936 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL306123 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2304017 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2304006 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2304015 | — | IC50 | = | 130.0 | nM | 6.89 |