Assay Detail
Binding
CHEMBL666579
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Inhibition of [3H]Leu-enkephalin binding to Dipeptidyl aminopeptidase (DAP)
12
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Retro-inverso concept applied to the complete inhibitors of enkephalin-degrading enzymes.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.97 | 9.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL85320 | KELATORPHAN | — | 1 | 9.05 |
| CHEMBL37418 | — | — | 1 | 8.60 |
| CHEMBL55056 | — | — | 1 | 7.76 |
| CHEMBL16779 | — | — | 1 | 7.68 |
| CHEMBL57623 | — | — | 1 | 7.49 |
| CHEMBL299588 | — | — | 2 | 7.15 |
| CHEMBL1907967 | — | — | 1 | 6.85 |
| CHEMBL1907791 | — | — | 1 | 6.35 |
| CHEMBL1907968 | — | — | 1 | 5.70 |
| CHEMBL17107 | — | — | 1 | 4.46 |
| CHEMBL1907790 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL85320 | KELATORPHAN | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL37418 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL55056 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL16779 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL57623 | — | IC50 | = | 32.5 | nM | 7.49 |
| CHEMBL299588 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL1907967 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL1907791 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1907968 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL299588 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL17107 | — | IC50 | = | 35000.0 | nM | 4.46 |
| CHEMBL1907790 | — | IC50 | ~ | 32000.0 | nM | - |