Assay Detail
Binding
CHEMBL3748890
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 2-((1E,3E,5E)-5-(1-Ethyl-3,3-dimethyl-5-sulfoindolin-2-ylidene)-penta-1,3-dien-1-yl)-1-(6-((6-((6S,7R,7aR,12bS)-9-hydroxy-7-methoxy-3-methyl-1,2,3,4,5,6,7,7a-octahydro-4a,7-ethano-4,12-methanobenzofuro[3,2-e]isoquinoline-6-carboxamido)hexyl)-amino)-6-oxohexyl)-3,3-dimethyl-3H-indol-1-ium-5-sulfonate,2,2,2-Trifluoroacetate Salt from human MOR expressed in HEK293 cells by Cheng-Prusoff 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 | 8.67 | 9.91 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | 2.0 | 1 | 9.91 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.56 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.94 |
| CHEMBL1618305 | NALOXONAZINE | — | 1 | 8.84 |
| CHEMBL278789 | DERMORPHIN | — | 1 | 7.71 |
| CHEMBL38874 | DAMGO | — | 1 | 7.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL281786 | DIPRENORPHINE | Ki | = | 0.123 | nM | 9.91 |
| CHEMBL19019 | NALTREXONE | Ki | = | 0.2754 | nM | 9.56 |
| CHEMBL80 | NALOXONE | Ki | = | 1.148 | nM | 8.94 |
| CHEMBL1618305 | NALOXONAZINE | Ki | = | 1.445 | nM | 8.84 |
| CHEMBL278789 | DERMORPHIN | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL38874 | DAMGO | Ki | = | 87.1 | nM | 7.06 |