Assay Detail
Functional
CHEMBL755509
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Inhibitory activity in stimulating [35S]-GTP-gamma S binding mediated by the Opioid receptor kappa 1 in chinese Hamster Ovary (CHO) cell membranes was determined
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design and synthesis of novel dimeric morphinan ligands for kappa and micro opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 8.41 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | — | 1 | 9.72 |
| CHEMBL147511 | — | — | 1 | 9.07 |
| CHEMBL301160 | BUTORPHAN | — | 1 | 8.89 |
| CHEMBL146756 | — | — | 1 | 8.64 |
| CHEMBL413512 | — | — | 1 | 8.48 |
| CHEMBL433697 | — | — | 1 | 8.35 |
| CHEMBL358104 | — | — | 1 | 8.31 |
| CHEMBL357334 | — | — | 1 | 8.24 |
| CHEMBL424328 | — | — | 1 | 8.09 |
| CHEMBL405131 | — | — | 1 | 7.96 |
| CHEMBL346436 | — | — | 1 | 7.82 |
| CHEMBL290543 | — | — | 1 | 7.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | EC50 | = | 0.19 | nM | 9.72 |
| CHEMBL147511 | — | EC50 | = | 0.85 | nM | 9.07 |
| CHEMBL301160 | BUTORPHAN | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL146756 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL413512 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL433697 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL358104 | — | EC50 | = | 4.9 | nM | 8.31 |
| CHEMBL357334 | — | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL424328 | — | EC50 | = | 8.1 | nM | 8.09 |
| CHEMBL405131 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL346436 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL290543 | — | EC50 | = | 46.0 | nM | 7.34 |