Assay Detail
Binding
CHEMBL679283
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Binding affinity against endothelin A receptor in MMQ cells in rat
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | MMQ |
| 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 | 15 | 9.19 | 10.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL339904 | — | — | 1 | 10.15 |
| CHEMBL129220 | — | — | 1 | 9.96 |
| CHEMBL336272 | — | — | 1 | 9.92 |
| CHEMBL340575 | — | — | 1 | 9.77 |
| CHEMBL112832 | — | — | 1 | 9.32 |
| CHEMBL110366 | — | — | 1 | 9.22 |
| CHEMBL128240 | — | — | 1 | 9.11 |
| CHEMBL113611 | — | — | 1 | 9.07 |
| CHEMBL129740 | — | — | 1 | 9.04 |
| CHEMBL128061 | — | — | 1 | 8.97 |
| CHEMBL326191 | — | — | 1 | 8.92 |
| CHEMBL340190 | — | — | 1 | 8.86 |
| CHEMBL419211 | — | — | 1 | 8.82 |
| CHEMBL339969 | — | — | 1 | 8.48 |
| CHEMBL129060 | — | — | 1 | 8.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL339904 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL129220 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL336272 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL340575 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL112832 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL110366 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL128240 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL113611 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL129740 | — | IC50 | = | 0.92 | nM | 9.04 |
| CHEMBL128061 | — | IC50 | = | 1.06 | nM | 8.97 |
| CHEMBL326191 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL340190 | — | IC50 | = | 1.38 | nM | 8.86 |
| CHEMBL419211 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL339969 | — | IC50 | = | 3.28 | nM | 8.48 |
| CHEMBL129060 | — | IC50 | = | 5.2 | nM | 8.28 |