Assay Detail
Binding
CHEMBL1046475
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Displacement of [125I]ET1 from endothelin B receptor in DBA mouse microsomes
7
Total Activities
7
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
PET-compatible endothelin receptor radioligands: synthesis and first in vitro and in vivo studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 7.24 | 8.90 |
| IC50 | 1 | 6.11 | 6.11 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL593928 | — | — | 1 | 8.90 |
| CHEMBL603635 | — | — | 1 | 7.14 |
| CHEMBL611626 | — | — | 1 | 7.02 |
| CHEMBL604286 | — | — | 1 | 7.01 |
| CHEMBL594265 | — | — | 1 | 6.77 |
| CHEMBL594482 | — | — | 1 | 6.62 |
| CHEMBL8981 | PD-156707 | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL593928 | — | Ki | = | 1.26 | nM | 8.90 |
| CHEMBL603635 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL611626 | — | Ki | = | 96.0 | nM | 7.02 |
| CHEMBL604286 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL594265 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL594482 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL8981 | PD-156707 | IC50 | = | 780.0 | nM | 6.11 |