Assay Detail
Functional
CHEMBL799771
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Compound was evaluated for the functional assay performed by obtaining ET-1 concentration-response curves [pA2(ETA)] in isolated rat aortic rings
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Aorta |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Endothelin antagonists: discovery of EMD 122946, a highly potent and orally active ETA selective antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 5 | 8.36 | 9.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL298725 | — | — | 1 | 9.50 |
| CHEMBL9194 | ATRASENTAN | 3.0 | 1 | 8.60 |
| CHEMBL48907 | — | — | 1 | 8.50 |
| CHEMBL48881 | — | — | 1 | 7.60 |
| CHEMBL25438 | PD-156707 SODIUM | — | 1 | 7.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL298725 | — | Kd | = | 0.3162 | nM | 9.50 |
| CHEMBL9194 | ATRASENTAN | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL48907 | — | Kd | = | 3.162 | nM | 8.50 |
| CHEMBL48881 | — | Kd | = | 25.12 | nM | 7.60 |
| CHEMBL25438 | PD-156707 SODIUM | Kd | = | 25.12 | nM | 7.60 |