Assay Detail
Binding
CHEMBL758225
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Affinity to mu-receptor, using [3H]DAMGO as radioligand in homogenates of guinea pig brain membranes
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 | 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 | 17 | 7.88 | 9.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1094879 | — | — | 1 | 9.44 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 9.17 |
| CHEMBL1095519 | — | — | 1 | 8.17 |
| CHEMBL2114291 | — | — | 1 | 4.72 |
| CHEMBL2114294 | — | — | 1 | - |
| CHEMBL94320 | — | — | 1 | - |
| CHEMBL2114292 | — | — | 1 | - |
| CHEMBL2114296 | — | — | 1 | - |
| CHEMBL2115272 | — | — | 1 | - |
| CHEMBL2114293 | — | — | 1 | - |
| CHEMBL97051 | — | — | 1 | - |
| CHEMBL97590 | — | — | 1 | - |
| CHEMBL2115271 | — | — | 1 | - |
| CHEMBL2115270 | — | — | 1 | - |
| CHEMBL319835 | — | — | 1 | - |
| CHEMBL2114295 | — | — | 1 | - |
| CHEMBL2115273 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1094879 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL80 | NALOXONE | Ki | = | 0.68 | nM | 9.17 |
| CHEMBL1095519 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL2114291 | — | Ki | = | 19100.0 | nM | 4.72 |
| CHEMBL2114294 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL94320 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2114292 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2114296 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2115272 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2114293 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL97051 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL97590 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2115271 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL2115270 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL319835 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2114295 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL2115273 | — | Ki | > | 1000.0 | nM | - |