Assay Detail
Binding
CHEMBL838864
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Inhibition of [3H]U-69593 binding to rat opioid receptor kappa 1 expressed in HEK 293 cells
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Studies toward the pharmacophore of salvinorin A, a potent kappa opioid receptor agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.23 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL445332 | SALVINORIN A | 1.0 | 1 | 8.40 |
| CHEMBL370678 | — | — | 1 | 8.22 |
| CHEMBL194545 | — | — | 1 | 8.22 |
| CHEMBL370680 | — | — | 1 | 7.75 |
| CHEMBL365533 | — | — | 1 | 7.75 |
| CHEMBL195344 | — | — | 1 | 7.23 |
| CHEMBL364058 | — | — | 1 | 6.81 |
| CHEMBL435108 | SALVINORIN A (ESTER) | — | 1 | 6.79 |
| CHEMBL425016 | — | — | 1 | 6.46 |
| CHEMBL365547 | — | — | 1 | 5.99 |
| CHEMBL237054 | 1-ALPHA-HYDROXYSALVINORIN A | — | 1 | 5.95 |
| CHEMBL191597 | — | — | 1 | - |
| CHEMBL363482 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL445332 | SALVINORIN A | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL370678 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL194545 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL370680 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL365533 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL195344 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL364058 | — | Ki | = | 156.0 | nM | 6.81 |
| CHEMBL435108 | SALVINORIN A (ESTER) | Ki | = | 163.0 | nM | 6.79 |
| CHEMBL425016 | — | Ki | = | 347.0 | nM | 6.46 |
| CHEMBL365547 | — | Ki | = | 1022.0 | nM | 5.99 |
| CHEMBL237054 | 1-ALPHA-HYDROXYSALVINORIN A | Ki | = | 1125.0 | nM | 5.95 |
| CHEMBL191597 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL363482 | — | Ki | > | 10000.0 | nM | - |