Assay Detail
Functional
CHEMBL5384101
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Inverse agonist activity at human DOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HTLA |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Binding Mechanism of Pyrazoloisoquinoline-Based Novel β-Arrestin Inverse Agonists of the Kappa-Opioid Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 6.62 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5439465 | — | — | 1 | 7.30 |
| CHEMBL5430894 | — | — | 1 | 6.68 |
| CHEMBL5395170 | — | — | 1 | 6.32 |
| CHEMBL5429274 | — | — | 1 | 6.16 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5439465 | — | EC50 | = | 49.5 | nM | 7.30 |
| CHEMBL5430894 | — | EC50 | = | 207.0 | nM | 6.68 |
| CHEMBL5395170 | — | EC50 | = | 483.0 | nM | 6.32 |
| CHEMBL5429274 | — | EC50 | = | 691.0 | nM | 6.16 |