Assay Detail
Functional
CHEMBL756054
Review assay metadata, readout intent, target linkage, and publication context from the same page.
The compound was tested for antagonist activity by selective inhibition of [35S]GTP-gamma-S, binding in Guinea pig caudate stimulated by U69,593 to Opioid receptor kappa 1
5
Total Activities
5
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
Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 9.23 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL52451 | — | — | 1 | 9.77 |
| CHEMBL300662 | — | — | 1 | 9.48 |
| CHEMBL50594 | — | — | 1 | 9.25 |
| CHEMBL51838 | — | — | 1 | 8.98 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.69 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL52451 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL300662 | — | Ki | = | 0.33 | nM | 9.48 |
| CHEMBL50594 | — | Ki | = | 0.567 | nM | 9.25 |
| CHEMBL51838 | — | Ki | = | 1.04 | nM | 8.98 |
| CHEMBL19019 | NALTREXONE | Ki | = | 2.06 | nM | 8.69 |