Assay Detail
Functional
CHEMBL5046496
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human mu opioid receptor expressed in HEK293T cells assessed as Galphai2 activation preincubated with compound in D-PBS for 3 hrs followed by coelenterazine addition for 5 mins once again compound addition for 10 mins by BRET assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel Dual-Target μ-Opioid Receptor and Dopamine D<sub>3</sub> Receptor Ligands as Potential Nonaddictive Pharmacotherapeutics for Pain Management.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 5.72 | 6.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL80 | NALOXONE | 4.0 | 1 | 6.52 |
| CHEMBL5077114 | — | — | 1 | 5.68 |
| CHEMBL5082465 | — | — | 1 | 5.45 |
| CHEMBL5086564 | — | — | 1 | 5.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL80 | NALOXONE | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL5077114 | — | IC50 | = | 2089.3 | nM | 5.68 |
| CHEMBL5082465 | — | IC50 | = | 3548.13 | nM | 5.45 |
| CHEMBL5086564 | — | IC50 | = | 5754.4 | nM | 5.24 |