Assay Detail
Binding
CHEMBL5736048
Review assay metadata, readout intent, target linkage, and publication context from the same page.
beta-Arrestin Assay: The DISCOVERX PATHHUNTER® β-Arrestin assay is used to measure β-arrestin-2 activity. The technology is based on Enzyme Fragment Complementation (EFC) with β-galactosidase (β-Gal) as the reporter. The enzyme is split into two inactive complementary portions (EA for Enzyme Acceptor, and ED for Enzyme Donor) expressed as fusion proteins in the cell. EA is fused to β-arrestin-2, and ED is fused to the C-terminus of the GPCR of interest. When a ligand binds and the GPCR is activated, β-arrestin-2 is recruited to the receptor resulting in an ED/EA complementation, restoring β-Gal activity, which is measured using chemiluminescence. For this assay, the PathHunter human OPRM1 (μ, MOR) Arrestin CHO-K1 cell line was used. The EMAX values of the chemiluminescent signal were all normalized to DAMGO, which is defined as 100%.
33
Total Activities
11
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Substituted 3-dialkylaminomethyl-piperidin-4-yl-benzamides and methods of making and using same
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 11 | 5.93 | 7.22 |
| kon | 11 | - | - |
| k_off | 11 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5739600 | — | — | 3 | 7.22 |
| CHEMBL5905642 | — | — | 3 | 6.57 |
| CHEMBL5665374 | — | — | 3 | 6.51 |
| CHEMBL5977166 | — | — | 3 | 6.08 |
| CHEMBL5895874 | — | — | 3 | 5.59 |
| CHEMBL5946750 | — | — | 3 | 5.51 |
| CHEMBL6052956 | — | — | 3 | 5.50 |
| CHEMBL5806020 | — | — | 3 | 5.43 |
| CHEMBL5809483 | — | — | 3 | 4.97 |
| CHEMBL6001487 | — | — | 3 | - |
| CHEMBL5959297 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5739600 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5905642 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL5665374 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL5977166 | — | EC50 | = | 830.0 | nM | 6.08 |
| CHEMBL5895874 | — | EC50 | = | 2560.0 | nM | 5.59 |
| CHEMBL5946750 | — | EC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL6052956 | — | EC50 | = | 3170.0 | nM | 5.50 |
| CHEMBL5806020 | — | EC50 | = | 3670.0 | nM | 5.43 |
| CHEMBL5809483 | — | EC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL5809483 | — | kon | = | - | — | - |
| CHEMBL5739600 | — | kon | = | - | — | - |
| CHEMBL5977166 | — | k_off | = | - | s-1 | - |
| CHEMBL5806020 | — | k_off | = | - | s-1 | - |
| CHEMBL5806020 | — | kon | = | - | — | - |
| CHEMBL6052956 | — | k_off | = | - | s-1 | - |
| CHEMBL6052956 | — | kon | = | - | — | - |
| CHEMBL5895874 | — | k_off | = | - | s-1 | - |
| CHEMBL5895874 | — | kon | = | - | — | - |
| CHEMBL5665374 | — | k_off | = | - | s-1 | - |
| CHEMBL5665374 | — | kon | = | - | — | - |
| CHEMBL5739600 | — | k_off | = | - | s-1 | - |
| CHEMBL5809483 | — | k_off | = | - | s-1 | - |
| CHEMBL5905642 | — | k_off | = | - | s-1 | - |
| CHEMBL5905642 | — | kon | = | - | — | - |
| CHEMBL5946750 | — | k_off | = | - | s-1 | - |
| CHEMBL5946750 | — | kon | = | - | — | - |
| CHEMBL5977166 | — | kon | = | - | — | - |
| CHEMBL5959297 | — | kon | = | - | — | - |
| CHEMBL5959297 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL6001487 | — | k_off | = | - | s-1 | - |
| CHEMBL6001487 | — | kon | = | - | — | - |
| CHEMBL6001487 | — | EC50 | > | 100000.0 | nM | - |
| CHEMBL5959297 | — | k_off | = | - | s-1 | - |