Assay Detail
Binding
CHEMBL5157652
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Displacement of [3H]-U69593 from KOR in guinea pig brain membranes measured by competitive radioligand receptor binding assay
16
Total Activities
16
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
Synthesis of 8-aminomorphans with high KOR affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.73 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL128444 | — | — | 1 | 9.62 |
| CHEMBL290543 | — | — | 1 | 9.47 |
| CHEMBL603370 | — | — | 1 | 9.34 |
| CHEMBL5175676 | — | — | 1 | 8.15 |
| CHEMBL5173028 | — | — | 1 | 8.15 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.14 |
| CHEMBL5178401 | — | — | 1 | 7.89 |
| CHEMBL5203422 | — | — | 1 | 7.75 |
| CHEMBL5200121 | — | — | 1 | 7.64 |
| CHEMBL5208146 | — | — | 1 | 7.58 |
| CHEMBL5196638 | — | — | 1 | 7.14 |
| CHEMBL5190238 | — | — | 1 | 6.91 |
| CHEMBL5204863 | — | — | 1 | 6.28 |
| CHEMBL5200869 | — | — | 1 | 6.06 |
| CHEMBL5185196 | — | — | 1 | 5.76 |
| CHEMBL5207267 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL128444 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL290543 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL603370 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL5175676 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL5173028 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL80 | NALOXONE | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL5178401 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL5203422 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL5200121 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL5208146 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL5196638 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL5190238 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL5204863 | — | Ki | = | 531.0 | nM | 6.28 |
| CHEMBL5200869 | — | Ki | = | 862.0 | nM | 6.06 |
| CHEMBL5185196 | — | Ki | = | 1750.0 | nM | 5.76 |
| CHEMBL5207267 | — | Ki | > | 1000.0 | nM | - |