Assay Detail
Binding
CHEMBL753527
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Binding affinity towards Opioid receptor kappa 1 expressed in CHO cells was determined by using [3H]diprenorphine 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 | 9.07 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL216640 | — | — | 1 | 9.85 |
| CHEMBL428669 | — | — | 1 | 9.80 |
| CHEMBL438781 | — | — | 1 | 9.70 |
| CHEMBL439272 | — | — | 1 | 9.68 |
| CHEMBL262963 | — | — | 1 | 9.59 |
| CHEMBL415795 | — | — | 1 | 9.47 |
| CHEMBL415330 | — | — | 1 | 9.41 |
| CHEMBL411282 | — | — | 1 | 9.34 |
| CHEMBL440449 | — | — | 1 | 9.07 |
| CHEMBL261992 | — | — | 1 | 8.96 |
| CHEMBL415818 | — | — | 1 | 8.90 |
| CHEMBL414904 | — | — | 1 | 8.88 |
| CHEMBL405721 | — | — | 1 | 8.87 |
| CHEMBL414360 | — | — | 1 | 8.81 |
| CHEMBL414477 | — | — | 1 | 8.80 |
| CHEMBL405307 | — | — | 1 | 8.65 |
| CHEMBL440810 | — | — | 1 | 8.27 |
| CHEMBL410152 | — | — | 1 | 8.21 |
| CHEMBL438044 | — | — | 1 | 8.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL216640 | — | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL428669 | — | Ki | = | 0.16 | nM | 9.80 |
| CHEMBL438781 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL439272 | — | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL262963 | — | Ki | = | 0.26 | nM | 9.59 |
| CHEMBL415795 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL415330 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL411282 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL440449 | — | Ki | = | 0.86 | nM | 9.07 |
| CHEMBL261992 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL415818 | — | Ki | = | 1.26 | nM | 8.90 |
| CHEMBL414904 | — | Ki | = | 1.33 | nM | 8.88 |
| CHEMBL405721 | — | Ki | = | 1.34 | nM | 8.87 |
| CHEMBL414360 | — | Ki | = | 1.56 | nM | 8.81 |
| CHEMBL414477 | — | Ki | = | 1.59 | nM | 8.80 |
| CHEMBL405307 | — | Ki | = | 2.25 | nM | 8.65 |
| CHEMBL440810 | — | Ki | = | 5.41 | nM | 8.27 |
| CHEMBL410152 | — | Ki | = | 6.12 | nM | 8.21 |
| CHEMBL438044 | — | Ki | = | 9.03 | nM | 8.04 |