Assay Detail
Binding
CHEMBL671334
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Ability to displace endothelin ([125I]ET-3) from endothelin B receptor derived from cerebellar tissue of porcine.
37
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 8.04 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL325581 | — | — | 2 | 9.70 |
| CHEMBL111277 | — | — | 2 | 9.54 |
| CHEMBL323464 | — | — | 2 | 9.49 |
| CHEMBL419367 | — | — | 2 | 9.49 |
| CHEMBL109644 | — | — | 2 | 9.47 |
| CHEMBL322297 | — | — | 1 | 8.92 |
| CHEMBL323055 | — | — | 1 | 8.80 |
| CHEMBL324639 | — | — | 1 | 8.59 |
| CHEMBL110700 | — | — | 1 | 8.54 |
| CHEMBL419749 | — | — | 1 | 8.39 |
| CHEMBL419383 | — | — | 1 | 8.35 |
| CHEMBL111712 | — | — | 1 | 8.28 |
| CHEMBL110899 | — | — | 1 | 8.28 |
| CHEMBL324214 | — | — | 1 | 8.20 |
| CHEMBL111010 | — | — | 1 | 8.15 |
| CHEMBL109765 | — | — | 1 | 8.03 |
| CHEMBL109408 | — | — | 1 | 7.47 |
| CHEMBL326861 | — | — | 1 | 7.44 |
| CHEMBL433842 | — | — | 1 | 7.39 |
| CHEMBL111517 | — | — | 1 | 7.24 |
| CHEMBL111355 | — | — | 1 | 7.22 |
| CHEMBL323789 | — | — | 1 | 7.21 |
| CHEMBL321035 | — | — | 1 | 7.18 |
| CHEMBL110305 | — | — | 1 | 7.17 |
| CHEMBL321673 | — | — | 1 | 7.14 |
| CHEMBL108748 | — | — | 1 | 7.11 |
| CHEMBL113087 | — | — | 1 | 7.07 |
| CHEMBL111769 | — | — | 1 | 7.02 |
| CHEMBL108142 | — | — | 1 | 6.68 |
| CHEMBL111728 | — | — | 1 | 6.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL325581 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL111277 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL419367 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL323464 | — | IC50 | = | 0.32 | nM | 9.49 |
| CHEMBL109644 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL111277 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL419367 | — | IC50 | = | 0.98 | nM | 9.01 |
| CHEMBL325581 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL323464 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL322297 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL109644 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL323055 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL324639 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL110700 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL419749 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL419383 | — | IC50 | = | 4.5 | nM | 8.35 |
| CHEMBL111712 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL110899 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL324214 | — | IC50 | = | 6.3 | nM | 8.20 |
| CHEMBL111010 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL109765 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL109408 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL326861 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL433842 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL111517 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL111355 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL323789 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL321035 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL110305 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL321673 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL108748 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL113087 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL111769 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL108142 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL111728 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL109242 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL111783 | — | IC50 | = | 850.0 | nM | 6.07 |