Assay Detail
Binding
CHEMBL1674427
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Displacement of [3H]U69593 from kappa opioid receptor in guinea pig cerebellum
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Cerebellum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis of 6,14-epoxymorphinan derivatives and their pharmacologies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 9.51 | 10.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1672473 | — | — | 1 | 10.12 |
| CHEMBL1672481 | — | — | 1 | 10.09 |
| CHEMBL1672484 | — | — | 1 | 10.08 |
| CHEMBL1672480 | — | — | 1 | 10.06 |
| CHEMBL1672478 | — | — | 1 | 9.97 |
| CHEMBL1672486 | — | — | 1 | 9.94 |
| CHEMBL1672470 | — | — | 1 | 9.92 |
| CHEMBL1672471 | — | — | 1 | 9.91 |
| CHEMBL1672468 | — | — | 1 | 9.90 |
| CHEMBL1672490 | — | — | 1 | 9.88 |
| CHEMBL1672469 | — | — | 1 | 9.88 |
| CHEMBL1672475 | — | — | 1 | 9.87 |
| CHEMBL1672487 | — | — | 1 | 9.85 |
| CHEMBL1672472 | — | — | 1 | 9.83 |
| CHEMBL267495 | NALFURAFINE | 4.0 | 1 | 9.65 |
| CHEMBL1672477 | — | — | 1 | 9.64 |
| CHEMBL1672474 | — | — | 1 | 9.49 |
| CHEMBL1672479 | — | — | 1 | 9.42 |
| CHEMBL1672494 | — | — | 1 | 9.36 |
| CHEMBL1672488 | — | — | 1 | 9.27 |
| CHEMBL1672492 | — | — | 1 | 9.16 |
| CHEMBL1672476 | — | — | 1 | 9.15 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 9.06 |
| CHEMBL1672482 | — | — | 1 | 8.98 |
| CHEMBL1672483 | — | — | 1 | 8.95 |
| CHEMBL1672491 | — | — | 1 | 8.95 |
| CHEMBL1672489 | — | — | 1 | 8.74 |
| CHEMBL1672485 | — | — | 1 | 8.64 |
| CHEMBL1672493 | — | — | 1 | 8.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1672473 | — | Ki | = | 0.0754 | nM | 10.12 |
| CHEMBL1672481 | — | Ki | = | 0.0812 | nM | 10.09 |
| CHEMBL1672484 | — | Ki | = | 0.0833 | nM | 10.08 |
| CHEMBL1672480 | — | Ki | = | 0.088 | nM | 10.06 |
| CHEMBL1672478 | — | Ki | = | 0.108 | nM | 9.97 |
| CHEMBL1672486 | — | Ki | = | 0.116 | nM | 9.94 |
| CHEMBL1672470 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL1672471 | — | Ki | = | 0.124 | nM | 9.91 |
| CHEMBL1672468 | — | Ki | = | 0.126 | nM | 9.90 |
| CHEMBL1672490 | — | Ki | = | 0.133 | nM | 9.88 |
| CHEMBL1672469 | — | Ki | = | 0.132 | nM | 9.88 |
| CHEMBL1672475 | — | Ki | = | 0.135 | nM | 9.87 |
| CHEMBL1672487 | — | Ki | = | 0.141 | nM | 9.85 |
| CHEMBL1672472 | — | Ki | = | 0.147 | nM | 9.83 |
| CHEMBL267495 | NALFURAFINE | Ki | = | 0.225 | nM | 9.65 |
| CHEMBL1672477 | — | Ki | = | 0.228 | nM | 9.64 |
| CHEMBL1672474 | — | Ki | = | 0.326 | nM | 9.49 |
| CHEMBL1672479 | — | Ki | = | 0.384 | nM | 9.42 |
| CHEMBL1672494 | — | Ki | = | 0.438 | nM | 9.36 |
| CHEMBL1672488 | — | Ki | = | 0.543 | nM | 9.27 |
| CHEMBL1672492 | — | Ki | = | 0.699 | nM | 9.16 |
| CHEMBL1672476 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 0.861 | nM | 9.06 |
| CHEMBL1672482 | — | Ki | = | 1.05 | nM | 8.98 |
| CHEMBL1672483 | — | Ki | = | 1.12 | nM | 8.95 |
| CHEMBL1672491 | — | Ki | = | 1.13 | nM | 8.95 |
| CHEMBL1672489 | — | Ki | = | 1.82 | nM | 8.74 |
| CHEMBL1672485 | — | Ki | = | 2.31 | nM | 8.64 |
| CHEMBL1672493 | — | Ki | = | 8.56 | nM | 8.07 |