Assay Detail
Binding
CHEMBL3370191
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-naloxone from rat mu opioid receptor expressed in HEK cells after 60 mins
8
Total Activities
8
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 | 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 |
|---|---|---|---|
| Ki | 8 | 6.45 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.70 |
| CHEMBL3325714 | — | — | 1 | 6.33 |
| CHEMBL3325715 | — | — | 1 | 6.21 |
| CHEMBL3325716 | — | — | 1 | 6.13 |
| CHEMBL3325719 | — | — | 1 | 5.89 |
| CHEMBL3325707 | — | — | 1 | 5.41 |
| CHEMBL3325841 | — | — | 1 | - |
| CHEMBL3325710 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL80 | NALOXONE | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL3325714 | — | Ki | = | 470.0 | nM | 6.33 |
| CHEMBL3325715 | — | Ki | = | 610.0 | nM | 6.21 |
| CHEMBL3325716 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL3325719 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL3325707 | — | Ki | = | 3930.0 | nM | 5.41 |
| CHEMBL3325841 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL3325710 | — | Ki | > | 100000.0 | nM | - |