Assay Detail
Functional
CHEMBL3370194
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human kappa opioid receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced cAMP production after 30 mins by HTRF assay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery, structure-activity relationship studies, and anti-nociceptive effects of 1-phenyl-3,6,6-trimethyl-1,5,6,7-tetrahydro-4H-indazol-4-one as novel opioid receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.69 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL290543 | — | — | 1 | 9.52 |
| CHEMBL3325716 | — | — | 1 | 6.43 |
| CHEMBL3325714 | — | — | 1 | 6.39 |
| CHEMBL3325715 | — | — | 1 | 6.24 |
| CHEMBL3325841 | — | — | 1 | 5.96 |
| CHEMBL3325713 | — | — | 1 | 5.58 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL290543 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3325716 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3325714 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL3325715 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL3325841 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3325713 | — | IC50 | = | 2650.0 | nM | 5.58 |