Assay Detail
Binding
CHEMBL900981
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DAMGO from rat mu-opioid receptor transfected in HN9.10 cells after 3 hrs
20
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.42 | 9.08 |
| Ki | 10 | 7.75 | 9.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL235109 | — | — | 2 | 9.42 |
| CHEMBL392206 | — | — | 2 | 8.96 |
| CHEMBL235107 | — | — | 2 | 8.92 |
| CHEMBL235743 | — | — | 2 | 8.55 |
| CHEMBL439026 | — | — | 2 | 8.24 |
| CHEMBL235106 | — | — | 2 | 7.85 |
| CHEMBL392207 | — | — | 2 | 7.64 |
| CHEMBL392185 | — | — | 2 | 7.40 |
| CHEMBL216239 | CARBOXYFENTANYL | — | 2 | 5.27 |
| CHEMBL235108 | — | — | 2 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL235109 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL235109 | — | IC50 | = | 0.8318 | nM | 9.08 |
| CHEMBL392206 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL235107 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL392206 | — | IC50 | = | 2.344 | nM | 8.63 |
| CHEMBL235107 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL235743 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL235743 | — | IC50 | = | 5.754 | nM | 8.24 |
| CHEMBL439026 | — | Ki | = | 5.7 | nM | 8.24 |
| CHEMBL439026 | — | IC50 | = | 12.02 | nM | 7.92 |
| CHEMBL235106 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL392207 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL235106 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL392185 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL392207 | — | IC50 | = | 57.54 | nM | 7.24 |
| CHEMBL392185 | — | IC50 | = | 89.13 | nM | 7.05 |
| CHEMBL216239 | CARBOXYFENTANYL | Ki | = | 5400.0 | nM | 5.27 |
| CHEMBL235108 | — | Ki | = | 5700.0 | nM | 5.24 |
| CHEMBL235108 | — | IC50 | = | 10964.78 | nM | 4.96 |
| CHEMBL216239 | CARBOXYFENTANYL | IC50 | = | 11748.98 | nM | 4.93 |