Assay Detail
Functional
CHEMBL5035605
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human MOR expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP accumulation incubated for 60 mins by cAMP HTRF assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of bifunctional piperidinamide derivatives as σ<sub>1</sub>R Antagonists/MOR agonists for treating neuropathic pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 4 | 8.18 | 9.14 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5087973 | — | — | 1 | 9.14 |
| CHEMBL5094951 | — | — | 1 | 8.64 |
| CHEMBL5079619 | — | — | 1 | 8.22 |
| CHEMBL5081955 | — | — | 1 | 6.72 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5087973 | — | EC50 | = | 0.73 | nM | 9.14 |
| CHEMBL5094951 | — | EC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5079619 | — | EC50 | = | 6.07 | nM | 8.22 |
| CHEMBL5081955 | — | EC50 | = | 189.9 | nM | 6.72 |