Assay Detail
Functional
CHEMBL4051335
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Agonist activity at human kappa-type opioid receptor expressed in CHO-K1 cells assessed as forskolin-induced cAMP accumulation after 30 mins in presence of forskolin by luminescence-based HitHunter cAMP assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Addressing Structural Flexibility at the A-Ring on Salvinorin A: Discovery of a Potent Kappa-Opioid Agonist with Enhanced Metabolic Stability.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 10 | 8.48 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL445332 | SALVINORIN A | 1.0 | 1 | 9.68 |
| CHEMBL4083444 | — | — | 1 | 9.22 |
| CHEMBL424698 | SALVINORIN B | — | 1 | 8.62 |
| CHEMBL4093687 | — | — | 1 | 7.93 |
| CHEMBL4094854 | — | — | 1 | 7.89 |
| CHEMBL4075281 | — | — | 1 | 7.52 |
| CHEMBL4076437 | — | — | 1 | - |
| CHEMBL4086641 | — | — | 1 | - |
| CHEMBL4105286 | — | — | 1 | - |
| CHEMBL1257853 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL445332 | SALVINORIN A | EC50 | = | 0.21 | nM | 9.68 |
| CHEMBL4083444 | — | EC50 | = | 0.6 | nM | 9.22 |
| CHEMBL424698 | SALVINORIN B | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL4093687 | — | EC50 | = | 11.7 | nM | 7.93 |
| CHEMBL4094854 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4075281 | — | EC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4076437 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4086641 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL4105286 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1257853 | — | EC50 | > | 10000.0 | nM | - |