Assay Detail
Binding
CHEMBL873580
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In vitro inhibition of [125I]ET1 binding to rat cerebellum Endothelin B receptor.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Cerebellum |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Selective endothelin A receptor antagonists. 3. Discovery and structure-activity relationships of a series of 4-phenoxybutanoic acid derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.07 | 5.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL330679 | — | — | 1 | 5.52 |
| CHEMBL90320 | — | — | 1 | 5.30 |
| CHEMBL91753 | — | — | 1 | 5.00 |
| CHEMBL96301 | — | — | 1 | 5.00 |
| CHEMBL92353 | — | — | 1 | 5.00 |
| CHEMBL329181 | — | — | 1 | 5.00 |
| CHEMBL93749 | — | — | 1 | 5.00 |
| CHEMBL92965 | — | — | 1 | 5.00 |
| CHEMBL94141 | — | — | 1 | 5.00 |
| CHEMBL93776 | — | — | 1 | 5.00 |
| CHEMBL93097 | — | — | 1 | 5.00 |
| CHEMBL93331 | — | — | 1 | 5.00 |
| CHEMBL327247 | — | — | 1 | - |
| CHEMBL421365 | — | — | 1 | - |
| CHEMBL93000 | — | — | 1 | - |
| CHEMBL314691 | BQ-123 | 2.0 | 1 | - |
| CHEMBL94279 | — | — | 1 | - |
| CHEMBL94071 | — | — | 1 | - |
| CHEMBL433209 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL330679 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL90320 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL91753 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL96301 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL92353 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL329181 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL93749 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL92965 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL94141 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL93776 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL93097 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL93331 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL327247 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL421365 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL93000 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL314691 | BQ-123 | IC50 | > | 30000.0 | nM | - |
| CHEMBL94279 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL94071 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL433209 | — | IC50 | > | 30000.0 | nM | - |