Assay Detail
Binding
CHEMBL3399797
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]diprenorphine from human recombinant mu opioid receptor expressed in HEK cells after 60 mins
8
Total Activities
8
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
Novel fluoroalkyl derivatives of selective kappa opioid receptor antagonist JDTic: Design, synthesis, pharmacology and molecular modeling studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 8 | 7.96 | 9.35 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.35 |
| CHEMBL415247 | JDTIC | 1.0 | 1 | 8.40 |
| CHEMBL3397593 | — | — | 1 | 7.88 |
| CHEMBL3397594 | — | — | 1 | 7.71 |
| CHEMBL3397596 | — | — | 1 | 7.24 |
| CHEMBL3397595 | — | — | 1 | 7.20 |
| CHEMBL58033 | (-)-U-50488 | — | 1 | - |
| CHEMBL31421 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL415247 | JDTIC | Ki | = | 4.0 | nM | 8.40 |
| CHEMBL3397593 | — | Ki | = | 13.23 | nM | 7.88 |
| CHEMBL3397594 | — | Ki | = | 19.61 | nM | 7.71 |
| CHEMBL3397596 | — | Ki | = | 57.52 | nM | 7.24 |
| CHEMBL3397595 | — | Ki | = | 63.08 | nM | 7.20 |
| CHEMBL58033 | (-)-U-50488 | Ki | - | — | - | |
| CHEMBL31421 | — | Ki | - | — | - |