Assay Detail
Binding
CHEMBL676491
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Ability to displace endothelin ([125I]ET1) from endothelin A receptor derived from MMQ cells of rodent.
37
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rodentia sp. |
| Cell Type | MMQ |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 8.89 | 10.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL325581 | — | — | 2 | 10.03 |
| CHEMBL323464 | — | — | 2 | 10.00 |
| CHEMBL109644 | — | — | 2 | 9.96 |
| CHEMBL111277 | — | — | 2 | 9.89 |
| CHEMBL323055 | — | — | 1 | 9.68 |
| CHEMBL419367 | — | — | 2 | 9.66 |
| CHEMBL419383 | — | — | 1 | 9.37 |
| CHEMBL322297 | — | — | 1 | 9.34 |
| CHEMBL321035 | — | — | 1 | 9.28 |
| CHEMBL419749 | — | — | 1 | 9.24 |
| CHEMBL111712 | — | — | 1 | 9.21 |
| CHEMBL111010 | — | — | 1 | 9.18 |
| CHEMBL110899 | — | — | 1 | 9.11 |
| CHEMBL111769 | — | — | 1 | 8.92 |
| CHEMBL324639 | — | — | 1 | 8.89 |
| CHEMBL108142 | — | — | 1 | 8.85 |
| CHEMBL326861 | — | — | 1 | 8.80 |
| CHEMBL111355 | — | — | 1 | 8.70 |
| CHEMBL324214 | — | — | 1 | 8.70 |
| CHEMBL109765 | — | — | 1 | 8.70 |
| CHEMBL321673 | — | — | 1 | 8.64 |
| CHEMBL110700 | — | — | 1 | 8.57 |
| CHEMBL111517 | — | — | 1 | 8.29 |
| CHEMBL108748 | — | — | 1 | 8.28 |
| CHEMBL433842 | — | — | 1 | 8.20 |
| CHEMBL323789 | — | — | 1 | 8.09 |
| CHEMBL113087 | — | — | 1 | 8.08 |
| CHEMBL109408 | — | — | 1 | 8.00 |
| CHEMBL111728 | — | — | 1 | 8.00 |
| CHEMBL110305 | — | — | 1 | 7.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL325581 | — | IC50 | = | 0.094 | nM | 10.03 |
| CHEMBL323464 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL109644 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL111277 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL323055 | — | IC50 | = | 0.21 | nM | 9.68 |
| CHEMBL419367 | — | IC50 | = | 0.22 | nM | 9.66 |
| CHEMBL325581 | — | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL419383 | — | IC50 | = | 0.43 | nM | 9.37 |
| CHEMBL322297 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL109644 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL111277 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL321035 | — | IC50 | = | 0.53 | nM | 9.28 |
| CHEMBL323464 | — | IC50 | = | 0.54 | nM | 9.27 |
| CHEMBL419367 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL419749 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL111712 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL111010 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL110899 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL111769 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL324639 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL108142 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL326861 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL324214 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL111355 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL109765 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL321673 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL110700 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL111517 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL108748 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL433842 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL323789 | — | IC50 | = | 8.1 | nM | 8.09 |
| CHEMBL113087 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL109408 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL111728 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL110305 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL111783 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL109242 | — | IC50 | = | 48.0 | nM | 7.32 |