Assay Detail
Functional
CHEMBL752837
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Inhibition of [35S]GTP-gamma-S, binding from Opioid receptor mu 1 in Guinea pig Caudate stimulated by DAMGO
4
Total Activities
4
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 an opioid kappa receptor subtype-selective N-substituent for (+)-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 4 | 8.84 | 10.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL150052 | — | — | 1 | 10.41 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.03 |
| CHEMBL10986 | — | — | 1 | 8.14 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 7.78 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL150052 | — | Ki | = | 0.039 | nM | 10.41 |
| CHEMBL19019 | NALTREXONE | Ki | = | 0.93 | nM | 9.03 |
| CHEMBL10986 | — | Ki | = | 7.25 | nM | 8.14 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 16.75 | nM | 7.78 |