Assay Detail
Binding
CHEMBL679708
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Inhibitory activity against 125 I-labeled ET-1 binding to Endothelin A receptor in porcine aortic smooth muscle membranes.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Synthesis of 2-substituted d-tryptophan-containing peptide derivatives with endothelin receptor antagonist activity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 7.18 | 8.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL284250 | — | — | 1 | 8.42 |
| CHEMBL289349 | — | — | 1 | 8.25 |
| CHEMBL289410 | — | — | 1 | 7.82 |
| CHEMBL314691 | BQ-123 | 2.0 | 1 | 7.66 |
| CHEMBL287888 | — | — | 1 | 6.75 |
| CHEMBL37807 | — | — | 1 | 6.55 |
| CHEMBL414175 | — | — | 1 | 6.32 |
| CHEMBL431124 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL284250 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL289349 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL289410 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL314691 | BQ-123 | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL287888 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL37807 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL414175 | — | IC50 | = | 474.0 | nM | 6.32 |
| CHEMBL431124 | — | IC50 | = | 2000.0 | nM | 5.70 |