Assay Detail
Binding
CHEMBL755522
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Displacement of [3H]U-69593 from kappa opioid receptors in guine pig brain (minus cerebellum).
21
Total Activities
18
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 | Intermediate |
Publication
(2S)-1-(arylacetyl)-2-(aminomethyl)piperidine derivatives: novel, highly selective kappa opioid analgesics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 21 | 8.33 | 9.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL71294 | — | — | 1 | 9.62 |
| CHEMBL130272 | — | — | 2 | 9.48 |
| CHEMBL128542 | — | — | 2 | 9.24 |
| CHEMBL131034 | — | — | 2 | 9.22 |
| CHEMBL2111856 | — | — | 1 | 9.15 |
| CHEMBL130125 | — | — | 1 | 9.08 |
| CHEMBL290543 | — | — | 1 | 9.01 |
| CHEMBL128631 | — | — | 1 | 8.97 |
| CHEMBL433849 | — | — | 1 | 8.89 |
| CHEMBL128766 | — | — | 1 | 8.78 |
| CHEMBL435391 | — | — | 1 | 8.74 |
| CHEMBL337841 | — | — | 1 | 8.42 |
| CHEMBL447782 | — | — | 1 | 8.07 |
| CHEMBL2111857 | — | — | 1 | 7.81 |
| CHEMBL128796 | — | — | 1 | 7.81 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.82 |
| CHEMBL128912 | — | — | 1 | 6.71 |
| CHEMBL130714 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL71294 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL130272 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL128542 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL131034 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2111856 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL128542 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL130125 | — | Ki | = | 0.84 | nM | 9.08 |
| CHEMBL290543 | — | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL128631 | — | Ki | = | 1.07 | nM | 8.97 |
| CHEMBL433849 | — | Ki | = | 1.28 | nM | 8.89 |
| CHEMBL128766 | — | Ki | = | 1.68 | nM | 8.78 |
| CHEMBL435391 | — | Ki | = | 1.83 | nM | 8.74 |
| CHEMBL337841 | — | Ki | = | 3.84 | nM | 8.42 |
| CHEMBL447782 | — | Ki | = | 8.54 | nM | 8.07 |
| CHEMBL130272 | — | Ki | = | 11.7 | nM | 7.93 |
| CHEMBL2111857 | — | Ki | = | 15.4 | nM | 7.81 |
| CHEMBL128796 | — | Ki | = | 15.4 | nM | 7.81 |
| CHEMBL70 | MORPHINE | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL128912 | — | Ki | = | 194.0 | nM | 6.71 |
| CHEMBL130714 | — | Ki | = | 827.0 | nM | 6.08 |
| CHEMBL131034 | — | Ki | = | 1000.0 | nM | 6.00 |