Assay Detail
Binding
CHEMBL900980
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Displacement of [3H]DPDPE from human delta-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 | Homo sapiens |
| 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 |
|---|---|---|---|
| Ki | 10 | 7.50 | 9.44 |
| IC50 | 10 | 7.17 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL235109 | — | — | 2 | 9.44 |
| CHEMBL392207 | — | — | 2 | 9.16 |
| CHEMBL439026 | — | — | 2 | 8.49 |
| CHEMBL235107 | — | — | 2 | 8.43 |
| CHEMBL392206 | — | — | 2 | 8.21 |
| CHEMBL235106 | — | — | 2 | 7.85 |
| CHEMBL392185 | — | — | 2 | 6.75 |
| CHEMBL235743 | — | — | 2 | 6.52 |
| CHEMBL235108 | — | — | 2 | 5.16 |
| CHEMBL216239 | CARBOXYFENTANYL | — | 2 | 5.03 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL235109 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL392207 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL235109 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL392207 | — | IC50 | = | 1.778 | nM | 8.75 |
| CHEMBL439026 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL235107 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL392206 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL439026 | — | IC50 | = | 6.607 | nM | 8.18 |
| CHEMBL235107 | — | IC50 | = | 7.586 | nM | 8.12 |
| CHEMBL392206 | — | IC50 | = | 13.18 | nM | 7.88 |
| CHEMBL235106 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL235106 | — | IC50 | = | 30.9 | nM | 7.51 |
| CHEMBL392185 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL235743 | — | Ki | = | 300.0 | nM | 6.52 |
| CHEMBL392185 | — | IC50 | = | 398.11 | nM | 6.40 |
| CHEMBL235743 | — | IC50 | = | 724.44 | nM | 6.14 |
| CHEMBL235108 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL216239 | CARBOXYFENTANYL | Ki | = | 9400.0 | nM | 5.03 |
| CHEMBL235108 | — | IC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL216239 | CARBOXYFENTANYL | IC50 | = | 19952.62 | nM | 4.70 |