Assay Detail
Binding
CHEMBL993515
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]norBNI from kappa opioid receptor expressed in CHO cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Publication
14-O-Heterocyclic-substituted naltrexone derivatives as non-peptide mu opioid receptor selective antagonists: design, synthesis, and biological studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.31 | 9.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL473136 | — | — | 1 | 9.03 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.29 |
| CHEMBL476600 | — | — | 1 | 7.59 |
| CHEMBL513990 | — | — | 1 | 7.33 |
| CHEMBL476603 | — | — | 1 | 7.32 |
| CHEMBL515621 | — | — | 1 | 7.31 |
| CHEMBL472843 | — | — | 1 | 7.17 |
| CHEMBL473253 | — | — | 1 | 6.83 |
| CHEMBL516263 | — | — | 1 | 6.23 |
| CHEMBL500766 | — | — | 1 | 6.00 |
| CHEMBL516085 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL473136 | — | Ki | = | 0.94 | nM | 9.03 |
| CHEMBL19019 | NALTREXONE | Ki | = | 5.15 | nM | 8.29 |
| CHEMBL476600 | — | Ki | = | 25.5 | nM | 7.59 |
| CHEMBL513990 | — | Ki | = | 46.57 | nM | 7.33 |
| CHEMBL476603 | — | Ki | = | 47.81 | nM | 7.32 |
| CHEMBL515621 | — | Ki | = | 49.21 | nM | 7.31 |
| CHEMBL472843 | — | Ki | = | 67.15 | nM | 7.17 |
| CHEMBL473253 | — | Ki | = | 148.23 | nM | 6.83 |
| CHEMBL516263 | — | Ki | = | 586.42 | nM | 6.23 |
| CHEMBL500766 | — | Ki | = | 1012.7 | nM | 6.00 |
| CHEMBL516085 | — | Ki | > | 10000.0 | nM | - |