Assay Detail
Functional
CHEMBL3227490
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human mu opioid receptor expressed in Gqi5 transfected CHO cells assessed as inhibition of DAMGO-stimulated Ca2+ influx preincubated for 15 mins followed by DAMGO challenge
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
A Bivalent Ligand Targeting the Putative Mu Opioid Receptor and Chemokine Receptor CCR5 Heterodimers: Binding Affinity versus Functional Activities.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 7.62 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.05 |
| CHEMBL3219778 | — | — | 1 | 7.42 |
| CHEMBL3219777 | — | — | 1 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | IC50 | = | 8.9 | nM | 8.05 |
| CHEMBL3219778 | — | IC50 | = | 37.8 | nM | 7.42 |
| CHEMBL3219777 | — | IC50 | = | 40.0 | nM | 7.40 |