Assay Detail
Binding
CHEMBL677314
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In vitro inhibition of enkephalinase purified from rat kidney.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
New bidentates as full inhibitors of enkephalin-degrading enzymes: synthesis and analgesic properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.46 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL275637 | — | — | 1 | 9.00 |
| CHEMBL16975 | — | — | 1 | 8.92 |
| CHEMBL16779 | — | — | 1 | 8.85 |
| CHEMBL16457 | — | — | 1 | 8.82 |
| CHEMBL16046 | — | — | 1 | 8.70 |
| CHEMBL10247 | THIORPHAN | -1.0 | 1 | 8.40 |
| CHEMBL16622 | — | — | 1 | 8.00 |
| CHEMBL17107 | — | — | 1 | 7.92 |
| CHEMBL274994 | — | — | 1 | 7.52 |
| CHEMBL17040 | — | — | 1 | 6.46 |
| CHEMBL16791 | — | — | 1 | 6.22 |
| CHEMBL17095 | — | — | 1 | 6.16 |
| CHEMBL16568 | — | — | 1 | 6.12 |
| CHEMBL16675 | — | — | 1 | 6.10 |
| CHEMBL16467 | — | — | 1 | 6.10 |
| CHEMBL17084 | — | — | 1 | 6.07 |
| CHEMBL17059 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL275637 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL16975 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL16779 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL16457 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL16046 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL10247 | THIORPHAN | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL16622 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL17107 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL274994 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL17040 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL16791 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL17095 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL16568 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL16675 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL16467 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL17084 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL17059 | — | IC50 | > | 1.0 | nM | - |