Assay Detail
Binding
CHEMBL5736047
Review assay metadata, readout intent, target linkage, and publication context from the same page.
G-Protein Assay: G-protein signaling was measured via second messenger cAMP modulation. Detection of cAMP modulation was accomplished in the PathHunter human OPRM1 (μ, MOR) Arrestin CHO-K1 cell line using the Dynamic2 cAMP Kit from Cisbio. The EMAX values of the chemiluminescent signal are 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 | 6.94 | 8.00 |
| kon | 11 | - | - |
| k_off | 11 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5905642 | — | — | 3 | 8.00 |
| CHEMBL5977166 | — | — | 3 | 7.47 |
| CHEMBL5665374 | — | — | 3 | 7.22 |
| CHEMBL6001487 | — | — | 3 | 7.17 |
| CHEMBL5895874 | — | — | 3 | 6.99 |
| CHEMBL5946750 | — | — | 3 | 6.80 |
| CHEMBL6052956 | — | — | 3 | 6.79 |
| CHEMBL5806020 | — | — | 3 | 6.33 |
| CHEMBL5959297 | — | — | 3 | 6.33 |
| CHEMBL5809483 | — | — | 3 | 6.26 |
| CHEMBL5739600 | — | — | 3 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5905642 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5977166 | — | EC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5665374 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL6001487 | — | EC50 | = | 67.0 | nM | 7.17 |
| CHEMBL5895874 | — | EC50 | = | 102.0 | nM | 6.99 |
| CHEMBL5946750 | — | EC50 | = | 160.0 | nM | 6.80 |
| CHEMBL6052956 | — | EC50 | = | 163.0 | nM | 6.79 |
| CHEMBL5806020 | — | EC50 | = | 463.0 | nM | 6.33 |
| CHEMBL5959297 | — | EC50 | = | 467.0 | nM | 6.33 |
| CHEMBL5809483 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5739600 | — | EC50 | < | 10.0 | nM | - |
| 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 | - |
| CHEMBL5739600 | — | kon | = | - | — | - |
| CHEMBL5977166 | — | k_off | = | - | s-1 | - |
| CHEMBL5809483 | — | kon | = | - | — | - |
| CHEMBL5905642 | — | k_off | = | - | s-1 | - |
| CHEMBL5905642 | — | kon | = | - | — | - |
| CHEMBL5946750 | — | k_off | = | - | s-1 | - |
| CHEMBL5946750 | — | kon | = | - | — | - |
| CHEMBL5977166 | — | kon | = | - | — | - |
| CHEMBL5959297 | — | kon | = | - | — | - |
| CHEMBL6001487 | — | k_off | = | - | s-1 | - |
| CHEMBL6001487 | — | kon | = | - | — | - |
| CHEMBL5809483 | — | k_off | = | - | s-1 | - |
| CHEMBL5959297 | — | k_off | = | - | s-1 | - |