Assay Detail
Binding
CHEMBL843957
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In Vitro inhibition of recombinant human endothelin converting enzyme-1
33
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Potent and selective non-peptidic inhibitors of endothelin-converting enzyme-1 with sustained duration of action.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 7.21 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL147964 | — | — | 2 | 8.59 |
| CHEMBL148056 | — | — | 1 | 8.22 |
| CHEMBL147157 | — | — | 1 | 8.19 |
| CHEMBL147847 | — | — | 1 | 8.10 |
| CHEMBL357226 | — | — | 1 | 7.89 |
| CHEMBL359024 | — | — | 2 | 7.85 |
| CHEMBL285619 | — | — | 1 | 7.77 |
| CHEMBL423751 | — | — | 2 | 7.72 |
| CHEMBL342962 | — | — | 1 | 7.66 |
| CHEMBL146936 | — | — | 1 | 7.66 |
| CHEMBL413724 | — | — | 1 | 7.64 |
| CHEMBL357251 | — | — | 2 | 7.62 |
| CHEMBL357441 | — | — | 2 | 7.54 |
| CHEMBL147163 | — | — | 1 | 7.52 |
| CHEMBL358098 | — | — | 2 | 7.46 |
| CHEMBL358774 | — | — | 1 | 7.40 |
| CHEMBL289150 | — | — | 1 | 7.29 |
| CHEMBL148232 | — | — | 1 | 7.19 |
| CHEMBL342077 | — | — | 2 | 7.02 |
| CHEMBL145943 | — | — | 1 | 7.01 |
| CHEMBL40028 | — | — | 1 | 6.82 |
| CHEMBL290698 | — | — | 1 | 6.39 |
| CHEMBL343904 | — | — | 1 | 6.28 |
| CHEMBL479579 | PHOSPHORAMIDON | — | 1 | 5.92 |
| CHEMBL147041 | — | — | 1 | - |
| CHEMBL10247 | THIORPHAN | -1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL147964 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL148056 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL147157 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL147847 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL357226 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL359024 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL285619 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL423751 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL342962 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL146936 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL413724 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL357251 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL357441 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL147163 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL358098 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL358774 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL289150 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL148232 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL342077 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL145943 | — | IC50 | = | 97.0 | nM | 7.01 |
| CHEMBL423751 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL40028 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL342077 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL359024 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL290698 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL147964 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL343904 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL358098 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL357441 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL479579 | PHOSPHORAMIDON | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL357251 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL147041 | — | IC50 | > | 4000.0 | nM | - |
| CHEMBL10247 | THIORPHAN | IC50 | > | 100000.0 | nM | - |