Assay Detail
Binding
CHEMBL756523
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity for the opioid receptor by displacement of tritiated naloxone from rat brain membranes.
26
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Subcellular | Membrane |
| Confidence | 4 — Cell-line / Tissue |
| 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 | 26 | 7.37 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL171763 | — | — | 1 | 10.00 |
| CHEMBL170805 | — | — | 1 | 9.30 |
| CHEMBL424952 | — | — | 1 | 9.22 |
| CHEMBL174176 | — | — | 1 | 8.89 |
| CHEMBL353806 | — | — | 1 | 8.54 |
| CHEMBL352616 | — | — | 1 | 8.00 |
| CHEMBL422900 | — | — | 1 | 7.77 |
| CHEMBL354641 | — | — | 1 | 7.75 |
| CHEMBL2110227 | — | — | 1 | 7.66 |
| CHEMBL170594 | — | — | 2 | 7.30 |
| CHEMBL311145 | — | — | 1 | 7.30 |
| CHEMBL354648 | — | — | 1 | 7.28 |
| CHEMBL423431 | — | — | 1 | 7.08 |
| CHEMBL170986 | — | — | 1 | 7.02 |
| CHEMBL414646 | — | — | 1 | 6.89 |
| CHEMBL2110336 | — | — | 1 | 6.85 |
| CHEMBL169855 | — | — | 1 | 6.82 |
| CHEMBL169183 | — | — | 1 | 6.82 |
| CHEMBL353292 | — | — | 1 | 6.80 |
| CHEMBL174125 | — | — | 1 | 6.55 |
| CHEMBL355563 | — | — | 1 | 6.54 |
| CHEMBL169252 | — | — | 1 | 6.52 |
| CHEMBL2110337 | — | — | 1 | 6.44 |
| CHEMBL173871 | — | — | 1 | 6.19 |
| CHEMBL2110228 | — | — | 1 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL171763 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL170805 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL424952 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL174176 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL353806 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL352616 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL422900 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL354641 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL2110227 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL170594 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL311145 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL354648 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL423431 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL170986 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL414646 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2110336 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL169855 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL169183 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL353292 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL174125 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL355563 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL169252 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL2110337 | — | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL170594 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL173871 | — | IC50 | = | 640.0 | nM | 6.19 |
| CHEMBL2110228 | — | IC50 | = | 1800.0 | nM | 5.75 |