Assay Detail
Binding
CHEMBL748034
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Inhibitory concentration was evaluated by Inhibiting 50% of Neutral endopeptidase enzyme (NEP) activity using 20 nM [3H]D-Ala2-Leu-enkephalin as substrate
16
Total Activities
16
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
Exploration of neutral endopeptidase active site by a series of new thiol-containing inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 7.40 | 8.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2110347 | — | — | 1 | 8.44 |
| CHEMBL10247 | THIORPHAN | -1.0 | 1 | 8.40 |
| CHEMBL55286 | — | — | 1 | 7.85 |
| CHEMBL174237 | — | — | 1 | 7.70 |
| CHEMBL171850 | — | — | 1 | 7.58 |
| CHEMBL2110258 | — | — | 1 | 7.46 |
| CHEMBL173287 | — | — | 1 | 7.43 |
| CHEMBL173919 | — | — | 1 | 7.40 |
| CHEMBL54601 | — | — | 1 | 7.36 |
| CHEMBL174066 | — | — | 1 | 7.30 |
| CHEMBL367174 | — | — | 1 | 7.30 |
| CHEMBL366937 | — | — | 1 | 7.30 |
| CHEMBL172787 | — | — | 1 | 7.28 |
| CHEMBL175110 | — | — | 1 | 6.75 |
| CHEMBL176960 | — | — | 1 | 6.50 |
| CHEMBL172978 | — | — | 1 | 6.42 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2110347 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL10247 | THIORPHAN | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL55286 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL174237 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL171850 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2110258 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL173287 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL173919 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL54601 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL174066 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL367174 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL366937 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL172787 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL175110 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL176960 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL172978 | — | IC50 | = | 380.0 | nM | 6.42 |