Assay Detail
Binding
CHEMBL1104716
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Displacement of [3H]Cl977 from human kappa opioid receptor expressed in HEK293 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.37 | 9.47 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 9.47 |
| CHEMBL290543 | — | — | 1 | 8.82 |
| CHEMBL1094880 | — | — | 1 | 8.22 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 7.83 |
| CHEMBL1095521 | — | — | 1 | 7.16 |
| CHEMBL1094237 | — | — | 1 | 6.92 |
| CHEMBL1096475 | — | — | 1 | 6.07 |
| CHEMBL1096473 | — | — | 1 | 6.04 |
| CHEMBL1096474 | — | — | 1 | 5.82 |
| CHEMBL1095184 | — | — | 1 | - |
| CHEMBL1094860 | — | — | 1 | - |
| CHEMBL1094236 | — | — | 1 | - |
| CHEMBL1095183 | — | — | 1 | - |
| CHEMBL1096675 | — | — | 1 | - |
| CHEMBL1095520 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL290543 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL1094880 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL80 | NALOXONE | Ki | = | 14.7 | nM | 7.83 |
| CHEMBL1095521 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL1094237 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1096475 | — | Ki | = | 850.0 | nM | 6.07 |
| CHEMBL1096473 | — | Ki | = | 920.0 | nM | 6.04 |
| CHEMBL1096474 | — | Ki | = | 1510.0 | nM | 5.82 |
| CHEMBL1095184 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1094860 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1094236 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1095183 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1096675 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1095520 | — | Ki | > | 1000.0 | nM | - |