Assay Detail
Binding
CHEMBL756660
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards Opioid receptor mu 1 expressed in CHO cells was determined by using[3H]DAMGO as radioligand
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and opioid activity of side-chain-to-side-chain cyclic dynorphin A-(1-11) amide analogues cyclized between positions 2 and 5. 1. Substitutions in position 3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.41 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL414477 | — | — | 1 | 9.66 |
| CHEMBL438781 | — | — | 1 | 9.59 |
| CHEMBL411282 | — | — | 1 | 9.28 |
| CHEMBL428669 | — | — | 1 | 8.93 |
| CHEMBL415330 | — | — | 1 | 8.73 |
| CHEMBL216640 | — | — | 1 | 8.72 |
| CHEMBL440449 | — | — | 1 | 8.70 |
| CHEMBL414904 | — | — | 1 | 8.68 |
| CHEMBL261992 | — | — | 1 | 8.60 |
| CHEMBL405721 | — | — | 1 | 8.47 |
| CHEMBL439272 | — | — | 1 | 8.41 |
| CHEMBL410152 | — | — | 1 | 8.38 |
| CHEMBL415818 | — | — | 1 | 8.34 |
| CHEMBL405307 | — | — | 1 | 8.14 |
| CHEMBL262963 | — | — | 1 | 7.79 |
| CHEMBL415795 | — | — | 1 | 7.70 |
| CHEMBL414360 | — | — | 1 | 7.37 |
| CHEMBL440810 | — | — | 1 | 7.34 |
| CHEMBL438044 | — | — | 1 | 6.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL414477 | — | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL438781 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL411282 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL428669 | — | Ki | = | 1.17 | nM | 8.93 |
| CHEMBL415330 | — | Ki | = | 1.88 | nM | 8.73 |
| CHEMBL216640 | — | Ki | = | 1.91 | nM | 8.72 |
| CHEMBL440449 | — | Ki | = | 2.02 | nM | 8.70 |
| CHEMBL414904 | — | Ki | = | 2.09 | nM | 8.68 |
| CHEMBL261992 | — | Ki | = | 2.52 | nM | 8.60 |
| CHEMBL405721 | — | Ki | = | 3.41 | nM | 8.47 |
| CHEMBL439272 | — | Ki | = | 3.89 | nM | 8.41 |
| CHEMBL410152 | — | Ki | = | 4.21 | nM | 8.38 |
| CHEMBL415818 | — | Ki | = | 4.57 | nM | 8.34 |
| CHEMBL405307 | — | Ki | = | 7.27 | nM | 8.14 |
| CHEMBL262963 | — | Ki | = | 16.4 | nM | 7.79 |
| CHEMBL415795 | — | Ki | = | 19.8 | nM | 7.70 |
| CHEMBL414360 | — | Ki | = | 42.7 | nM | 7.37 |
| CHEMBL440810 | — | Ki | = | 45.9 | nM | 7.34 |
| CHEMBL438044 | — | Ki | = | 125.0 | nM | 6.90 |