Assay Detail
Binding
CHEMBL679843
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Inhibitory activity against human bronchiolar smooth muscle Endothelin-converting enzyme 1
25
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Muscle tissue |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Hydroxamic acids as potent inhibitors of endothelin-converting enzyme from human bronchiolar smooth muscle.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 7.44 | 11.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL66284 | — | — | 1 | 11.00 |
| CHEMBL66967 | — | — | 1 | 9.70 |
| CHEMBL303159 | — | — | 1 | 9.60 |
| CHEMBL479579 | PHOSPHORAMIDON | — | 1 | 9.10 |
| CHEMBL63317 | — | — | 1 | 8.92 |
| CHEMBL304939 | — | — | 1 | 8.52 |
| CHEMBL303892 | — | — | 1 | 8.32 |
| CHEMBL67000 | — | — | 1 | 8.17 |
| CHEMBL85320 | KELATORPHAN | — | 1 | 8.10 |
| CHEMBL10247 | THIORPHAN | -1.0 | 1 | 8.10 |
| CHEMBL2372437 | — | — | 1 | 7.96 |
| CHEMBL68128 | — | — | 2 | 7.77 |
| CHEMBL67348 | — | — | 1 | 6.82 |
| CHEMBL69793 | — | — | 1 | 6.72 |
| CHEMBL65903 | — | — | 1 | 6.30 |
| CHEMBL69745 | — | — | 1 | 5.52 |
| CHEMBL66712 | — | — | 1 | 5.52 |
| CHEMBL308333 | ACTINONIN | — | 1 | 5.40 |
| CHEMBL66318 | — | — | 1 | 5.19 |
| CHEMBL68017 | — | — | 1 | 5.00 |
| CHEMBL2369423 | — | — | 1 | 4.48 |
| CHEMBL304736 | — | — | 1 | - |
| CHEMBL304496 | — | — | 1 | - |
| CHEMBL66882 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL66284 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL66967 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL303159 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL479579 | PHOSPHORAMIDON | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL63317 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL304939 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL303892 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL67000 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL85320 | KELATORPHAN | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL10247 | THIORPHAN | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL2372437 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL68128 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL68128 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL67348 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL69793 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL65903 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL69745 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL66712 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL308333 | ACTINONIN | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL66318 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL68017 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL2369423 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL304736 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL304496 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL66882 | — | IC50 | > | 10000.0 | nM | - |