Assay Detail
Binding
CHEMBL677268
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Ability to displace endothelin ([125I]ET1) from human Endothelin B receptor
5
Total Activities
5
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Pyrrolidine-3-carboxylic acids as endothelin antagonists. 2. Sulfonamide-based ETA/ETB mixed antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 7.06 | 7.75 |
| IC50 | 2 | 7.63 | 8.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL8978 | L-754142 | — | 1 | 8.36 |
| CHEMBL8823 | SB-209670 | — | 1 | 7.75 |
| CHEMBL431651 | ENRASENTAN | 2.0 | 1 | 6.96 |
| CHEMBL1205177 | — | — | 1 | 6.89 |
| CHEMBL957 | BOSENTAN | 4.0 | 1 | 6.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL8978 | L-754142 | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL8823 | SB-209670 | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL431651 | ENRASENTAN | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL1205177 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL957 | BOSENTAN | Ki | = | 340.0 | nM | 6.47 |