Assay Detail
Binding
CHEMBL682109
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Binding affinity towards Endothelin A receptor in human neuroblastoma-derived cell line SK-N-MC membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | SK-N-MC |
| 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 | 7 | 7.43 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2304015 | — | — | 1 | 8.54 |
| CHEMBL307936 | — | — | 1 | 8.52 |
| CHEMBL305524 | — | — | 1 | 8.19 |
| CHEMBL2304006 | — | — | 1 | 8.07 |
| CHEMBL73925 | — | — | 1 | 7.89 |
| CHEMBL306123 | — | — | 1 | 5.62 |
| CHEMBL2304017 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2304015 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL307936 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL305524 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL2304006 | — | IC50 | = | 8.6 | nM | 8.07 |
| CHEMBL73925 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL306123 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL2304017 | — | IC50 | = | 6200.0 | nM | 5.21 |