Assay Detail
Binding
CHEMBL753902
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory concentration was evaluated against kappa opioid receptor by displacement of tritiated U-69593 from rat brain membranes
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Enkephalin analogs as systemically active antinociceptive agents: O- and N-alkylated derivatives of the dipeptide amide L-2,6-dimethyltyrosyl-N-(3-phenylpropyl)-D-alaninamide.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 5.63 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL171763 | — | — | 1 | 6.66 |
| CHEMBL2110229 | — | — | 1 | 6.50 |
| CHEMBL353943 | — | — | 1 | 6.00 |
| CHEMBL169183 | — | — | 1 | 5.86 |
| CHEMBL2110337 | — | — | 1 | 5.60 |
| CHEMBL354641 | — | — | 1 | 4.97 |
| CHEMBL2110227 | — | — | 1 | 4.76 |
| CHEMBL170594 | — | — | 1 | 4.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL171763 | — | IC50 | = | 221.0 | nM | 6.66 |
| CHEMBL2110229 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL353943 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL169183 | — | IC50 | = | 1375.0 | nM | 5.86 |
| CHEMBL2110337 | — | IC50 | = | 2520.0 | nM | 5.60 |
| CHEMBL354641 | — | IC50 | = | 10800.0 | nM | 4.97 |
| CHEMBL2110227 | — | IC50 | = | 17470.0 | nM | 4.76 |
| CHEMBL170594 | — | IC50 | = | 19763.0 | nM | 4.70 |