Assay Detail
Binding
CHEMBL676101
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Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Thoracic aorta |
| Cell Type | A10 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of monocyclic endothelin analogs
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 11 | 6.79 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL437472 | ENDOTHELIN | 2.0 | 1 | 9.82 |
| CHEMBL263581 | — | — | 1 | 8.68 |
| CHEMBL412346 | — | — | 1 | 7.29 |
| CHEMBL438470 | — | — | 1 | 6.89 |
| CHEMBL386629 | — | — | 1 | 6.73 |
| CHEMBL268318 | — | — | 1 | 6.19 |
| CHEMBL407887 | — | — | 1 | 6.03 |
| CHEMBL410001 | — | — | 1 | 5.51 |
| CHEMBL125377 | — | — | 1 | 5.41 |
| CHEMBL409578 | — | — | 1 | 5.32 |
| CHEMBL1790883 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL437472 | ENDOTHELIN | Kd | = | 0.15 | nM | 9.82 |
| CHEMBL263581 | — | Kd | = | 2.109 | nM | 8.68 |
| CHEMBL412346 | — | Kd | = | 51.9 | nM | 7.29 |
| CHEMBL438470 | — | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL386629 | — | Kd | = | 188.0 | nM | 6.73 |
| CHEMBL268318 | — | Kd | = | 646.0 | nM | 6.19 |
| CHEMBL407887 | — | Kd | = | 929.0 | nM | 6.03 |
| CHEMBL410001 | — | Kd | = | 3074.0 | nM | 5.51 |
| CHEMBL125377 | — | Kd | = | 3920.0 | nM | 5.41 |
| CHEMBL409578 | — | Kd | = | 4778.0 | nM | 5.32 |
| CHEMBL1790883 | — | Kd | > | 20000.0 | nM | - |