Assay Detail
Functional
CHEMBL864222
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Stimulation of [35S]GTP-gamma-S binding to human recombinant KOR
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effect of substitution in the aromatic ring of cinnamoylaminomorphinones and codeinones.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 9 | 8.19 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113666 | — | — | 1 | 10.00 |
| CHEMBL607125 | — | — | 1 | 9.70 |
| CHEMBL611400 | — | — | 1 | 8.74 |
| CHEMBL607017 | — | — | 1 | 8.25 |
| CHEMBL607016 | — | — | 1 | 8.07 |
| CHEMBL611139 | — | — | 1 | 8.05 |
| CHEMBL607069 | — | — | 1 | 7.46 |
| CHEMBL607127 | — | — | 1 | 7.08 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113666 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL607125 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL611400 | — | EC50 | = | 1.8 | nM | 8.74 |
| CHEMBL607017 | — | EC50 | = | 5.6 | nM | 8.25 |
| CHEMBL607016 | — | EC50 | = | 8.5 | nM | 8.07 |
| CHEMBL611139 | — | EC50 | = | 9.0 | nM | 8.05 |
| CHEMBL607069 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL607127 | — | EC50 | = | 84.0 | nM | 7.08 |
| CHEMBL70 | MORPHINE | EC50 | = | 484.0 | nM | 6.32 |