Assay Detail
Binding
CHEMBL1006332
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]norBNI from monocloned kappa opioid receptor expressed in CHO cells
19
Total Activities
19
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
Design, synthesis, and biological evaluation of 6alpha- and 6beta-N-heterocyclic substituted naltrexamine derivatives as mu opioid receptor selective antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 7.71 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL495057 | — | — | 1 | 9.24 |
| CHEMBL473136 | — | — | 1 | 9.03 |
| CHEMBL521854 | — | — | 1 | 8.80 |
| CHEMBL523382 | — | — | 1 | 8.74 |
| CHEMBL494854 | — | — | 1 | 8.30 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.29 |
| CHEMBL472937 | — | — | 1 | 8.27 |
| CHEMBL271815 | — | — | 1 | 8.11 |
| CHEMBL494853 | — | — | 1 | 8.01 |
| CHEMBL515864 | — | — | 1 | 7.71 |
| CHEMBL522201 | — | — | 1 | 7.58 |
| CHEMBL271797 | — | — | 1 | 7.38 |
| CHEMBL522143 | — | — | 1 | 7.22 |
| CHEMBL493846 | — | — | 1 | 7.18 |
| CHEMBL514769 | — | — | 1 | 7.11 |
| CHEMBL514781 | — | — | 1 | 6.65 |
| CHEMBL260528 | — | — | 1 | 6.56 |
| CHEMBL495058 | — | — | 1 | 6.22 |
| CHEMBL525046 | — | — | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL495057 | — | Ki | = | 0.57 | nM | 9.24 |
| CHEMBL473136 | — | Ki | = | 0.94 | nM | 9.03 |
| CHEMBL521854 | — | Ki | = | 1.58 | nM | 8.80 |
| CHEMBL523382 | — | Ki | = | 1.81 | nM | 8.74 |
| CHEMBL494854 | — | Ki | = | 5.04 | nM | 8.30 |
| CHEMBL19019 | NALTREXONE | Ki | = | 5.15 | nM | 8.29 |
| CHEMBL472937 | — | Ki | = | 5.42 | nM | 8.27 |
| CHEMBL271815 | — | Ki | = | 7.79 | nM | 8.11 |
| CHEMBL494853 | — | Ki | = | 9.84 | nM | 8.01 |
| CHEMBL515864 | — | Ki | = | 19.56 | nM | 7.71 |
| CHEMBL522201 | — | Ki | = | 26.45 | nM | 7.58 |
| CHEMBL271797 | — | Ki | = | 41.69 | nM | 7.38 |
| CHEMBL522143 | — | Ki | = | 60.72 | nM | 7.22 |
| CHEMBL493846 | — | Ki | = | 65.26 | nM | 7.18 |
| CHEMBL514769 | — | Ki | = | 77.23 | nM | 7.11 |
| CHEMBL514781 | — | Ki | = | 222.58 | nM | 6.65 |
| CHEMBL260528 | — | Ki | = | 277.96 | nM | 6.56 |
| CHEMBL495058 | — | Ki | = | 608.76 | nM | 6.22 |
| CHEMBL525046 | — | Ki | = | 1012.7 | nM | 6.00 |