Assay Detail
Binding
CHEMBL755104
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Inhibitory activity against big ET-1 of Neutral endopeptidase
18
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Hydroxamic acids as potent inhibitors of endothelin-converting enzyme from human bronchiolar smooth muscle.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.69 | 10.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL66967 | — | — | 1 | 10.52 |
| CHEMBL303159 | — | — | 1 | 10.15 |
| CHEMBL66284 | — | — | 1 | 9.00 |
| CHEMBL479579 | PHOSPHORAMIDON | — | 1 | 8.70 |
| CHEMBL63317 | — | — | 1 | 8.52 |
| CHEMBL303892 | — | — | 1 | 8.15 |
| CHEMBL85320 | KELATORPHAN | — | 1 | 8.10 |
| CHEMBL67000 | — | — | 1 | 8.10 |
| CHEMBL10247 | THIORPHAN | -1.0 | 1 | 7.70 |
| CHEMBL304939 | — | — | 1 | 7.70 |
| CHEMBL68128 | — | — | 2 | 7.52 |
| CHEMBL2372437 | — | — | 1 | 7.40 |
| CHEMBL69793 | — | — | 1 | 6.57 |
| CHEMBL67348 | — | — | 1 | 6.12 |
| CHEMBL65903 | — | — | 1 | 6.00 |
| CHEMBL2369423 | — | — | 1 | 5.64 |
| CHEMBL308333 | ACTINONIN | — | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL66967 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL303159 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL66284 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL479579 | PHOSPHORAMIDON | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL63317 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL303892 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL85320 | KELATORPHAN | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL67000 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL10247 | THIORPHAN | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL304939 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL68128 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL2372437 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL68128 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL69793 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL67348 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL65903 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL2369423 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL308333 | ACTINONIN | IC50 | = | 8200.0 | nM | 5.09 |