Assay Detail
Binding
CHEMBL755003
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Affinity to opioid receptor kappa 1 using [3H]U-69593 as radioligand in homogenates of guinea pig brain membranes
19
Total Activities
19
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 | Intermediate |
Publication
Methylated analogues of methyl (R)-4-(3,4-dichlorophenylacetyl)- 3-(pyrrolidin-1-ylmethyl)piperazine-1-carboxylate (GR-89,696) as highly potent kappa-receptor agonists: stereoselective synthesis, opioid-receptor affinity, receptor selectivity, and functional studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.01 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1094879 | — | — | 1 | 9.51 |
| CHEMBL277863 | — | — | 1 | 9.35 |
| CHEMBL290543 | — | — | 1 | 9.31 |
| CHEMBL2114291 | — | — | 1 | 9.17 |
| CHEMBL1095519 | — | — | 1 | 8.62 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.49 |
| CHEMBL2115273 | — | — | 1 | 8.38 |
| CHEMBL2114295 | — | — | 1 | 8.06 |
| CHEMBL2114293 | — | — | 1 | 7.89 |
| CHEMBL2114294 | — | — | 1 | 7.46 |
| CHEMBL2114296 | — | — | 1 | 7.36 |
| CHEMBL97051 | — | — | 1 | 6.87 |
| CHEMBL2115271 | — | — | 1 | 6.69 |
| CHEMBL319835 | — | — | 1 | 6.62 |
| CHEMBL2114292 | — | — | 1 | 6.30 |
| CHEMBL2115272 | — | — | 1 | - |
| CHEMBL97590 | — | — | 1 | - |
| CHEMBL94320 | — | — | 1 | - |
| CHEMBL2115270 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1094879 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL277863 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL290543 | — | Ki | = | 0.49 | nM | 9.31 |
| CHEMBL2114291 | — | Ki | = | 0.67 | nM | 9.17 |
| CHEMBL1095519 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL80 | NALOXONE | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL2115273 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL2114295 | — | Ki | = | 8.8 | nM | 8.06 |
| CHEMBL2114293 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2114294 | — | Ki | = | 34.9 | nM | 7.46 |
| CHEMBL2114296 | — | Ki | = | 43.4 | nM | 7.36 |
| CHEMBL97051 | — | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL2115271 | — | Ki | = | 206.0 | nM | 6.69 |
| CHEMBL319835 | — | Ki | = | 237.0 | nM | 6.62 |
| CHEMBL2114292 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL2115272 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL97590 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL94320 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2115270 | — | Ki | > | 10000.0 | nM | - |