Assay Detail
Functional
CHEMBL755435
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Inhibition of stimulation of [35S]GTP-gamma-S, binding produced by the selective agonist (SNC-80, delta-receptor), in guinea pig caudate membranes
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
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 | 3 | 7.17 | 7.99 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 7.99 |
| CHEMBL10986 | — | — | 1 | 6.35 |
| CHEMBL51204 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL10986 | — | Ki | = | 450.0 | nM | 6.35 |
| CHEMBL51204 | — | Ki | > | 300.0 | nM | - |