Assay Detail
Binding
CHEMBL1924792
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]diprenorphine from human opioid kappa receptor expressed in CHO cells after 120 mins by scintillation counting
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 8.80 | 10.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL415247 | JDTIC | 1.0 | 1 | 10.23 |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 9.81 |
| CHEMBL575508 | — | — | 1 | 9.81 |
| CHEMBL277863 | — | — | 1 | 9.30 |
| CHEMBL1921845 | — | — | 1 | 9.25 |
| CHEMBL1921841 | — | — | 1 | 9.21 |
| CHEMBL1921844 | — | — | 1 | 9.21 |
| CHEMBL1921842 | — | — | 1 | 9.14 |
| CHEMBL1921847 | ATICAPRANT | 3.0 | 1 | 9.02 |
| CHEMBL1921850 | — | — | 1 | 8.98 |
| CHEMBL1921849 | — | — | 1 | 8.85 |
| CHEMBL1921840 | — | — | 1 | 8.83 |
| CHEMBL238316 | — | — | 1 | 8.75 |
| CHEMBL1921839 | — | — | 1 | 8.04 |
| CHEMBL1921848 | — | — | 1 | 7.85 |
| CHEMBL1921851 | — | — | 1 | 7.57 |
| CHEMBL1921843 | — | — | 1 | 7.35 |
| CHEMBL1921846 | — | — | 1 | 7.27 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL415247 | JDTIC | Ki | = | 0.0591 | nM | 10.23 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 0.153 | nM | 9.81 |
| CHEMBL575508 | — | Ki | = | 0.153 | nM | 9.81 |
| CHEMBL277863 | — | Ki | = | 0.502 | nM | 9.30 |
| CHEMBL1921845 | — | Ki | = | 0.565 | nM | 9.25 |
| CHEMBL1921841 | — | Ki | = | 0.622 | nM | 9.21 |
| CHEMBL1921844 | — | Ki | = | 0.617 | nM | 9.21 |
| CHEMBL1921842 | — | Ki | = | 0.722 | nM | 9.14 |
| CHEMBL1921847 | ATICAPRANT | Ki | = | 0.949 | nM | 9.02 |
| CHEMBL1921850 | — | Ki | = | 1.05 | nM | 8.98 |
| CHEMBL1921849 | — | Ki | = | 1.41 | nM | 8.85 |
| CHEMBL1921840 | — | Ki | = | 1.49 | nM | 8.83 |
| CHEMBL238316 | — | Ki | = | 1.78 | nM | 8.75 |
| CHEMBL1921839 | — | Ki | = | 9.21 | nM | 8.04 |
| CHEMBL1921848 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL1921851 | — | Ki | = | 26.7 | nM | 7.57 |
| CHEMBL1921843 | — | Ki | = | 44.9 | nM | 7.35 |
| CHEMBL1921846 | — | Ki | = | 53.7 | nM | 7.27 |