Assay Detail
Binding
CHEMBL675453
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Inhibition of Endothelin-converting enzyme (ECE) from microsomal fractions of bovine cultured endothelial cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Bos taurus |
| Cell Type | Endothelial cell |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Aminophosphonate endothelin converting enzyme inhibitors: potency-enhancing and selectivity-improving modifications of phosphoramidon
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 5.60 | 6.58 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL25269 | — | — | 1 | 6.58 |
| CHEMBL281562 | — | — | 1 | 6.02 |
| CHEMBL277199 | — | — | 1 | 5.96 |
| CHEMBL22509 | — | — | 1 | 5.82 |
| CHEMBL283758 | — | — | 1 | 5.72 |
| CHEMBL281785 | — | — | 1 | 5.55 |
| CHEMBL282663 | — | — | 1 | 5.52 |
| CHEMBL479579 | PHOSPHORAMIDON | — | 1 | 5.51 |
| CHEMBL281333 | — | — | 1 | 5.47 |
| CHEMBL277195 | — | — | 1 | 5.15 |
| CHEMBL280917 | — | — | 1 | 5.13 |
| CHEMBL279255 | — | — | 1 | 4.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL25269 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL281562 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL277199 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL22509 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL283758 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL281785 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL282663 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL479579 | PHOSPHORAMIDON | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL281333 | — | IC50 | = | 3400.0 | nM | 5.47 |
| CHEMBL277195 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL280917 | — | IC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL279255 | — | IC50 | = | 15000.0 | nM | 4.82 |