Assay Detail
Functional
CHEMBL4814801
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Agonist activity at mouse FLAG-tagged kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production preincubated for 20 mins followed by forskolin stimulation and measured after 15 mins by Glo-sensor reagent based assay
11
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Mus musculus |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Isolation and Pharmacological Characterization of Six Opioidergic <i>Picralima nitida</i> Alkaloids.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 6.46 | 8.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL290543 | — | — | 2 | 8.90 |
| CHEMBL4871880 | — | — | 1 | 7.14 |
| CHEMBL508955 | AKUAMMICINE | — | 2 | 6.62 |
| CHEMBL4852987 | — | — | 2 | 5.71 |
| CHEMBL4874877 | — | — | 2 | 5.60 |
| CHEMBL4846243 | — | — | 2 | 5.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL290543 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL290543 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL4871880 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL508955 | AKUAMMICINE | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL508955 | AKUAMMICINE | IC50 | = | 251.19 | nM | 6.60 |
| CHEMBL4852987 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL4852987 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4874877 | — | IC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4874877 | — | IC50 | = | 2710.0 | nM | 5.57 |
| CHEMBL4846243 | — | IC50 | = | 6309.57 | nM | 5.20 |
| CHEMBL4846243 | — | IC50 | = | 6460.0 | nM | 5.19 |