Assay Detail
Binding
CHEMBL877477
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Binding affinity towards human Endothelin B receptor by measuring its ability to displace [125I]ET-3 from guinea pig cerebellum
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebellum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Discovery and optimization of a novel class of orally active nonpeptidic endothelin-A receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 5.96 | 7.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL305980 | — | — | 1 | 7.24 |
| CHEMBL305270 | — | — | 1 | 6.80 |
| CHEMBL302753 | — | — | 1 | 6.71 |
| CHEMBL304721 | — | — | 1 | 6.01 |
| CHEMBL303034 | — | — | 1 | 6.00 |
| CHEMBL25344 | — | — | 1 | 6.00 |
| CHEMBL418326 | — | — | 1 | 5.96 |
| CHEMBL65833 | — | — | 1 | 5.89 |
| CHEMBL64009 | — | — | 1 | 5.89 |
| CHEMBL303390 | — | — | 1 | 5.89 |
| CHEMBL304173 | — | — | 1 | 5.85 |
| CHEMBL66402 | — | — | 1 | 5.82 |
| CHEMBL67084 | — | — | 1 | 5.77 |
| CHEMBL67536 | — | — | 1 | 5.75 |
| CHEMBL306218 | — | — | 1 | 5.72 |
| CHEMBL66893 | — | — | 1 | 5.60 |
| CHEMBL304778 | — | — | 1 | 5.60 |
| CHEMBL63648 | — | — | 1 | 5.46 |
| CHEMBL303501 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL305980 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL305270 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL302753 | — | Ki | = | 195.0 | nM | 6.71 |
| CHEMBL304721 | — | Ki | = | 970.0 | nM | 6.01 |
| CHEMBL303034 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL25344 | — | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL418326 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL65833 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL64009 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL303390 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL304173 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL66402 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL67084 | — | Ki | = | 1700.0 | nM | 5.77 |
| CHEMBL67536 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL306218 | — | Ki | = | 1900.0 | nM | 5.72 |
| CHEMBL66893 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL304778 | — | Ki | = | 2500.0 | nM | 5.60 |
| CHEMBL63648 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL303501 | — | Ki | = | 6000.0 | nM | 5.22 |