Assay Detail
Functional
CHEMBL758070
Review assay metadata, readout intent, target linkage, and publication context from the same page.
inhibition of stimulation of [35S]GTP-gamma-S, binding produced by the selective agonist (DAMGO, mu-receptor), in guinea pig caudate membranes
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 2 | 7.96 | 8.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL10986 | — | — | 1 | 8.14 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 7.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL10986 | — | Ki | = | 7.25 | nM | 8.14 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 16.7 | nM | 7.78 |