Assay Detail
Binding
CHEMBL646469
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Inhibition of dipeptidyl amino peptidase activity in rat brain with 10 nM [3H]Leu-enkephalin as substrate
16
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Brain |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
New kelatorphan-related inhibitors of enkephalin metabolism: improved antinociceptive properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.03 | 9.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2114408 | — | — | 1 | 9.34 |
| CHEMBL36094 | — | — | 2 | 9.05 |
| CHEMBL290366 | — | — | 1 | 8.64 |
| CHEMBL37418 | — | — | 1 | 8.60 |
| CHEMBL290337 | — | — | 1 | 8.60 |
| CHEMBL2114407 | — | — | 1 | 8.59 |
| CHEMBL2115347 | — | — | 1 | 8.14 |
| CHEMBL285617 | — | — | 2 | 7.98 |
| CHEMBL16779 | — | — | 1 | 7.68 |
| CHEMBL37921 | — | — | 1 | 7.64 |
| CHEMBL2115348 | — | — | 1 | 7.54 |
| CHEMBL440104 | — | — | 1 | 7.44 |
| CHEMBL417878 | — | — | 1 | 6.82 |
| CHEMBL36841 | — | — | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2114408 | — | IC50 | = | 0.46 | nM | 9.34 |
| CHEMBL36094 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL290366 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL37418 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL290337 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL2114407 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL2115347 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL36094 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL285617 | — | IC50 | = | 10.5 | nM | 7.98 |
| CHEMBL285617 | — | IC50 | = | 17.5 | nM | 7.76 |
| CHEMBL16779 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL37921 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2115348 | — | IC50 | = | 28.5 | nM | 7.54 |
| CHEMBL440104 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL417878 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL36841 | — | IC50 | = | 250.0 | nM | 6.60 |