Assay Detail
Binding
CHEMBL678073
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Inhibitory activity against human Endothelin A receptor in chinese hamster ovary cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
2,4-Diarylpyrrolidine-3-carboxylic acids--potent ETA selective endothelin receptor antagonists. 1. Discovery of A-127722.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 9.05 | 10.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL9194 | ATRASENTAN | 3.0 | 1 | 10.47 |
| CHEMBL8923 | — | — | 1 | 10.16 |
| CHEMBL8978 | L-754142 | — | 1 | 9.89 |
| CHEMBL8981 | PD-156707 | — | 1 | 9.77 |
| CHEMBL8823 | SB-209670 | — | 1 | 9.37 |
| CHEMBL428661 | — | — | 1 | 8.19 |
| CHEMBL267458 | BMS-182874 | — | 1 | 7.32 |
| CHEMBL428504 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL9194 | ATRASENTAN | Ki | = | 0.034 | nM | 10.47 |
| CHEMBL8923 | — | Ki | = | 0.069 | nM | 10.16 |
| CHEMBL8978 | L-754142 | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL8981 | PD-156707 | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL8823 | SB-209670 | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL428661 | — | Ki | = | 6.5 | nM | 8.19 |
| CHEMBL267458 | BMS-182874 | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL428504 | — | Ki | = | 63.0 | nM | 7.20 |