Assay Detail
Binding
CHEMBL1104714
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]U69593 from kappa opioid receptor in guinea pig brain membrane after 150 mins by scintillation counting
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| 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 | 17 | 7.82 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL290543 | — | — | 1 | 9.51 |
| CHEMBL1094879 | — | — | 1 | 9.51 |
| CHEMBL440765 | U-69593 | — | 1 | 9.01 |
| CHEMBL1094880 | — | — | 1 | 9.00 |
| CHEMBL1095519 | — | — | 1 | 8.62 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.14 |
| CHEMBL1095521 | — | — | 1 | 8.06 |
| CHEMBL1094237 | — | — | 1 | 7.89 |
| CHEMBL1096475 | — | — | 1 | 7.10 |
| CHEMBL1096675 | — | — | 1 | 6.82 |
| CHEMBL1096473 | — | — | 1 | 6.82 |
| CHEMBL1096474 | — | — | 1 | 6.38 |
| CHEMBL1094236 | — | — | 1 | 6.33 |
| CHEMBL1095183 | — | — | 1 | 6.29 |
| CHEMBL1095184 | — | — | 1 | - |
| CHEMBL1094860 | — | — | 1 | - |
| CHEMBL1095520 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL290543 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL1094879 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL440765 | U-69593 | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL1094880 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL1095519 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL80 | NALOXONE | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL1095521 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL1094237 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL1096475 | — | Ki | = | 80.0 | nM | 7.10 |
| CHEMBL1096675 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL1096473 | — | Ki | = | 152.0 | nM | 6.82 |
| CHEMBL1096474 | — | Ki | = | 421.0 | nM | 6.38 |
| CHEMBL1094236 | — | Ki | = | 464.0 | nM | 6.33 |
| CHEMBL1095183 | — | Ki | = | 515.0 | nM | 6.29 |
| CHEMBL1095184 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1094860 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1095520 | — | Ki | > | 1000.0 | nM | - |