Assay Detail
Binding
CHEMBL755105
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Inhibition of neutral endopeptidase activity in rabbit kidney with 20 nM [3H]D-Ala2-Leu-enkephalin as substrate
16
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
New kelatorphan-related inhibitors of enkephalin metabolism: improved antinociceptive properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.24 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL16779 | — | — | 1 | 8.85 |
| CHEMBL36094 | — | — | 2 | 8.77 |
| CHEMBL290337 | — | — | 1 | 8.74 |
| CHEMBL37921 | — | — | 1 | 8.64 |
| CHEMBL440104 | — | — | 1 | 8.62 |
| CHEMBL37418 | — | — | 1 | 8.60 |
| CHEMBL2114407 | — | — | 1 | 8.54 |
| CHEMBL2115347 | — | — | 1 | 8.52 |
| CHEMBL2114408 | — | — | 1 | 8.52 |
| CHEMBL2115348 | — | — | 1 | 8.12 |
| CHEMBL285617 | — | — | 2 | 7.89 |
| CHEMBL417878 | — | — | 1 | 7.56 |
| CHEMBL36841 | — | — | 1 | 7.29 |
| CHEMBL290366 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL16779 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL36094 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL290337 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL36094 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL37921 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL440104 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL37418 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2114407 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL2115347 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2114408 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL2115348 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL285617 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL285617 | — | IC50 | = | 26.5 | nM | 7.58 |
| CHEMBL417878 | — | IC50 | = | 27.5 | nM | 7.56 |
| CHEMBL36841 | — | IC50 | = | 51.5 | nM | 7.29 |
| CHEMBL290366 | — | IC50 | = | 150.0 | nM | 6.82 |