Assay Detail
Functional
CHEMBL887467
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Activity at human kappa opioid receptor expressed in HEK293 cells as intracellular calcium mobilization
10
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Convenient synthesis and in vitro pharmacological activity of 2-thioanalogs of salvinorins A and B.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 5 | 7.58 | 8.55 |
| Emax | 5 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL445332 | SALVINORIN A | 1.0 | 4 | 8.55 |
| CHEMBL231537 | 2-EPI-2-THIOSALVINORIN A | — | 2 | 6.91 |
| CHEMBL231536 | 2-THIOSALVINORIN B | — | 2 | 6.54 |
| CHEMBL231638 | 2-EPI-2-THIOSALVINORIN B | — | 2 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL445332 | SALVINORIN A | EC50 | = | 2.82 | nM | 8.55 |
| CHEMBL445332 | SALVINORIN A | EC50 | = | 4.77 | nM | 8.32 |
| CHEMBL231537 | 2-EPI-2-THIOSALVINORIN A | EC50 | = | 123.0 | nM | 6.91 |
| CHEMBL231536 | 2-THIOSALVINORIN B | EC50 | = | 287.0 | nM | 6.54 |
| CHEMBL231638 | 2-EPI-2-THIOSALVINORIN B | EC50 | > | 2000.0 | nM | - |
| CHEMBL445332 | SALVINORIN A | Emax | = | 100.0 | % | - |
| CHEMBL231536 | 2-THIOSALVINORIN B | Emax | = | 89.0 | % | - |
| CHEMBL445332 | SALVINORIN A | Emax | = | 107.0 | % | - |
| CHEMBL231537 | 2-EPI-2-THIOSALVINORIN A | Emax | = | 106.0 | % | - |
| CHEMBL231638 | 2-EPI-2-THIOSALVINORIN B | Emax | = | 71.0 | % | - |