Assay Detail
Binding
CHEMBL752824
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Inhibition of [3H]Ala2-Leu-enkephalin binding to Neutral endopeptidase (NEP)
14
Total Activities
13
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
Retro-inverso concept applied to the complete inhibitors of enkephalin-degrading enzymes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.42 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1907967 | — | — | 1 | 9.30 |
| CHEMBL16779 | — | — | 1 | 8.85 |
| CHEMBL55056 | — | — | 1 | 8.80 |
| CHEMBL85320 | KELATORPHAN | — | 1 | 8.77 |
| CHEMBL1907791 | — | — | 1 | 8.60 |
| CHEMBL37418 | — | — | 1 | 8.60 |
| CHEMBL57623 | — | — | 1 | 8.43 |
| CHEMBL17107 | — | — | 1 | 7.92 |
| CHEMBL299588 | — | — | 2 | 6.50 |
| CHEMBL1907793 | — | — | 1 | 5.76 |
| CHEMBL1907968 | — | — | 1 | 5.60 |
| CHEMBL1907790 | — | — | 1 | 5.47 |
| CHEMBL1907792 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1907967 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL16779 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL55056 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL85320 | KELATORPHAN | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1907791 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL37418 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL57623 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL17107 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL299588 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL299588 | — | IC50 | = | 945.0 | nM | 6.03 |
| CHEMBL1907793 | — | IC50 | = | 1730.0 | nM | 5.76 |
| CHEMBL1907968 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1907790 | — | IC50 | = | 3350.0 | nM | 5.47 |
| CHEMBL1907792 | — | IC50 | = | 6070.0 | nM | 5.22 |