Assay Detail
Binding
CHEMBL3748906
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]DAMGO from human MOR expressed in HEK293 cells preincubated for 1 hr followed by radioligand addition measured after 1 hr by liquid scintillation counting analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis, Biological Evaluation, and Utility of Fluorescent Ligands Targeting the μ-Opioid Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 6 | 9.08 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | 2.0 | 1 | 9.70 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.70 |
| CHEMBL38874 | DAMGO | — | 1 | 8.90 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.90 |
| CHEMBL278789 | DERMORPHIN | — | 1 | 8.80 |
| CHEMBL1618305 | NALOXONAZINE | — | 1 | 8.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL19019 | NALTREXONE | Ki | = | 0.1995 | nM | 9.70 |
| CHEMBL38874 | DAMGO | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL80 | NALOXONE | Ki | = | 1.259 | nM | 8.90 |
| CHEMBL278789 | DERMORPHIN | Ki | = | 1.585 | nM | 8.80 |
| CHEMBL1618305 | NALOXONAZINE | Ki | = | 3.162 | nM | 8.50 |