Assay Detail
Functional
CHEMBL1769427
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Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as [35S]GTPgammaS binding by scintillation counting
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 | Autocuration |
Publication
Aminothiazolomorphinans with mixed κ and μ opioid activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 7.69 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | — | 1 | 9.70 |
| CHEMBL242756 | — | — | 1 | 8.62 |
| CHEMBL1766023 | — | — | 1 | 7.85 |
| CHEMBL1766024 | — | — | 1 | 7.85 |
| CHEMBL1766041 | — | — | 1 | 7.66 |
| CHEMBL390866 | — | — | 1 | 7.54 |
| CHEMBL1766022 | — | — | 1 | 7.50 |
| CHEMBL58033 | (-)-U-50488 | — | 1 | 7.34 |
| CHEMBL1766036 | — | — | 1 | 7.34 |
| CHEMBL1766043 | — | — | 1 | 7.05 |
| CHEMBL1766025 | — | — | 1 | 6.92 |
| CHEMBL1766026 | — | — | 1 | 6.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL49269 | CYCLORPHAN | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL242756 | — | EC50 | = | 2.4 | nM | 8.62 |
| CHEMBL1766023 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1766024 | — | EC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1766041 | — | EC50 | = | 22.0 | nM | 7.66 |
| CHEMBL390866 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1766022 | — | EC50 | = | 32.0 | nM | 7.50 |
| CHEMBL58033 | (-)-U-50488 | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL1766036 | — | EC50 | = | 46.0 | nM | 7.34 |
| CHEMBL1766043 | — | EC50 | = | 89.0 | nM | 7.05 |
| CHEMBL1766025 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL1766026 | — | EC50 | = | 120.0 | nM | 6.92 |