Assay Detail
Functional
CHEMBL887394
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Agonist activity at huma kappa opioid receptor expressed in CHO cells assessed as U50488-stimulated of [35S]GTP-gamma-S binding
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
High-affinity carbamate analogues of morphinan at opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 8.44 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | — | 1 | 9.72 |
| CHEMBL397035 | — | — | 1 | 9.42 |
| CHEMBL263096 | — | — | 1 | 8.96 |
| CHEMBL427862 | — | — | 1 | 8.92 |
| CHEMBL301160 | BUTORPHAN | — | 1 | 8.89 |
| CHEMBL242048 | — | — | 1 | 8.66 |
| CHEMBL394624 | — | — | 1 | 8.33 |
| CHEMBL242046 | — | — | 1 | 8.02 |
| CHEMBL241824 | — | — | 1 | 7.80 |
| CHEMBL242047 | — | — | 1 | 7.64 |
| CHEMBL245049 | — | — | 1 | 7.54 |
| CHEMBL290543 | — | — | 1 | 7.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | EC50 | = | 0.19 | nM | 9.72 |
| CHEMBL397035 | — | EC50 | = | 0.38 | nM | 9.42 |
| CHEMBL263096 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL427862 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL301160 | BUTORPHAN | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL242048 | — | EC50 | = | 2.2 | nM | 8.66 |
| CHEMBL394624 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL242046 | — | EC50 | = | 9.6 | nM | 8.02 |
| CHEMBL241824 | — | EC50 | = | 16.0 | nM | 7.80 |
| CHEMBL242047 | — | EC50 | = | 23.0 | nM | 7.64 |
| CHEMBL245049 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL290543 | — | EC50 | = | 46.0 | nM | 7.34 |