Assay Detail
Functional
CHEMBL5384098
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inverse agonist activity at human KOR expressed in human HTLA cells assessed as beta arrestin-2 recruitment by ONE-Glo luciferase assay
17
Total Activities
17
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 | 17 | 6.84 | 8.04 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5439465 | — | — | 1 | 8.04 |
| CHEMBL5430894 | — | — | 1 | 8.03 |
| CHEMBL71294 | — | — | 1 | 7.98 |
| CHEMBL5423808 | — | — | 1 | 7.26 |
| CHEMBL5429274 | — | — | 1 | 7.16 |
| CHEMBL5430253 | — | — | 1 | 7.03 |
| CHEMBL5414202 | — | — | 1 | 6.99 |
| CHEMBL5418514 | — | — | 1 | 6.98 |
| CHEMBL5395170 | — | — | 1 | 6.90 |
| CHEMBL5429939 | — | — | 1 | 6.64 |
| CHEMBL5400992 | — | — | 1 | 6.47 |
| CHEMBL5393874 | — | — | 1 | 6.47 |
| CHEMBL5436422 | — | — | 1 | 6.37 |
| CHEMBL5400250 | — | — | 1 | 6.19 |
| CHEMBL5418213 | — | — | 1 | 6.17 |
| CHEMBL5407033 | — | — | 1 | 5.97 |
| CHEMBL5432768 | — | — | 1 | 5.57 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5439465 | — | EC50 | = | 9.1 | nM | 8.04 |
| CHEMBL5430894 | — | EC50 | = | 9.33 | nM | 8.03 |
| CHEMBL71294 | — | EC50 | = | 10.5 | nM | 7.98 |
| CHEMBL5423808 | — | EC50 | = | 54.5 | nM | 7.26 |
| CHEMBL5429274 | — | EC50 | = | 69.9 | nM | 7.16 |
| CHEMBL5430253 | — | EC50 | = | 94.3 | nM | 7.03 |
| CHEMBL5414202 | — | EC50 | = | 103.0 | nM | 6.99 |
| CHEMBL5418514 | — | EC50 | = | 105.0 | nM | 6.98 |
| CHEMBL5395170 | — | EC50 | = | 127.0 | nM | 6.90 |
| CHEMBL5429939 | — | EC50 | = | 227.0 | nM | 6.64 |
| CHEMBL5400992 | — | EC50 | = | 339.0 | nM | 6.47 |
| CHEMBL5393874 | — | EC50 | = | 338.0 | nM | 6.47 |
| CHEMBL5436422 | — | EC50 | = | 430.0 | nM | 6.37 |
| CHEMBL5400250 | — | EC50 | = | 643.0 | nM | 6.19 |
| CHEMBL5418213 | — | EC50 | = | 674.0 | nM | 6.17 |
| CHEMBL5407033 | — | EC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL5432768 | — | EC50 | = | 2670.0 | nM | 5.57 |