Assay Detail
Binding
CHEMBL673048
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Binding affinity against endothelin B receptor in porcine cerebellar tissue
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Sus scrofa |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 5. Highly selective, potent, and orally active ET(A) antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 5.74 | 7.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL339904 | — | — | 1 | 7.52 |
| CHEMBL129220 | — | — | 1 | 6.52 |
| CHEMBL9194 | ATRASENTAN | 3.0 | 1 | 6.29 |
| CHEMBL326191 | — | — | 1 | 6.02 |
| CHEMBL113611 | — | — | 1 | 6.01 |
| CHEMBL340190 | — | — | 1 | 5.98 |
| CHEMBL128061 | — | — | 1 | 5.95 |
| CHEMBL340575 | — | — | 1 | 5.89 |
| CHEMBL336272 | — | — | 1 | 5.67 |
| CHEMBL110366 | — | — | 1 | 5.57 |
| CHEMBL112832 | — | — | 1 | 5.29 |
| CHEMBL129060 | — | — | 1 | 5.11 |
| CHEMBL419211 | — | — | 1 | 5.10 |
| CHEMBL129740 | — | — | 1 | 5.09 |
| CHEMBL128240 | — | — | 1 | 4.92 |
| CHEMBL339969 | — | — | 1 | 4.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL339904 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL129220 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL9194 | ATRASENTAN | IC50 | = | 515.0 | nM | 6.29 |
| CHEMBL326191 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL113611 | — | IC50 | = | 984.0 | nM | 6.01 |
| CHEMBL340190 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL128061 | — | IC50 | = | 1130.0 | nM | 5.95 |
| CHEMBL340575 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL336272 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL110366 | — | IC50 | = | 2670.0 | nM | 5.57 |
| CHEMBL112832 | — | IC50 | = | 5080.0 | nM | 5.29 |
| CHEMBL129060 | — | IC50 | = | 7700.0 | nM | 5.11 |
| CHEMBL419211 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL129740 | — | IC50 | = | 8130.0 | nM | 5.09 |
| CHEMBL128240 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL339969 | — | IC50 | = | 14300.0 | nM | 4.84 |