Assay Detail
Binding
CHEMBL1006331
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Displacement of [3H]NTI from monocloned delta 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 | 7.03 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL494854 | — | — | 1 | 8.41 |
| CHEMBL495057 | — | — | 1 | 7.93 |
| CHEMBL521854 | — | — | 1 | 7.81 |
| CHEMBL473136 | — | — | 1 | 7.56 |
| CHEMBL493846 | — | — | 1 | 7.53 |
| CHEMBL523382 | — | — | 1 | 7.49 |
| CHEMBL514769 | — | — | 1 | 7.39 |
| CHEMBL514781 | — | — | 1 | 7.19 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 6.93 |
| CHEMBL522201 | — | — | 1 | 6.88 |
| CHEMBL494853 | — | — | 1 | 6.83 |
| CHEMBL515864 | — | — | 1 | 6.73 |
| CHEMBL472937 | — | — | 1 | 6.72 |
| CHEMBL260528 | — | — | 1 | 6.67 |
| CHEMBL522143 | — | — | 1 | 6.56 |
| CHEMBL271797 | — | — | 1 | 6.41 |
| CHEMBL271815 | — | — | 1 | 6.32 |
| CHEMBL495058 | — | — | 1 | 6.29 |
| CHEMBL525046 | — | — | 1 | 5.84 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL494854 | — | Ki | = | 3.86 | nM | 8.41 |
| CHEMBL495057 | — | Ki | = | 11.61 | nM | 7.93 |
| CHEMBL521854 | — | Ki | = | 15.42 | nM | 7.81 |
| CHEMBL473136 | — | Ki | = | 27.78 | nM | 7.56 |
| CHEMBL493846 | — | Ki | = | 29.26 | nM | 7.53 |
| CHEMBL523382 | — | Ki | = | 32.19 | nM | 7.49 |
| CHEMBL514769 | — | Ki | = | 40.78 | nM | 7.39 |
| CHEMBL514781 | — | Ki | = | 64.46 | nM | 7.19 |
| CHEMBL19019 | NALTREXONE | Ki | = | 117.06 | nM | 6.93 |
| CHEMBL522201 | — | Ki | = | 132.5 | nM | 6.88 |
| CHEMBL494853 | — | Ki | = | 148.2 | nM | 6.83 |
| CHEMBL515864 | — | Ki | = | 186.64 | nM | 6.73 |
| CHEMBL472937 | — | Ki | = | 191.98 | nM | 6.72 |
| CHEMBL260528 | — | Ki | = | 215.18 | nM | 6.67 |
| CHEMBL522143 | — | Ki | = | 277.51 | nM | 6.56 |
| CHEMBL271797 | — | Ki | = | 385.84 | nM | 6.41 |
| CHEMBL271815 | — | Ki | = | 478.82 | nM | 6.32 |
| CHEMBL495058 | — | Ki | = | 518.32 | nM | 6.29 |
| CHEMBL525046 | — | Ki | = | 1441.0 | nM | 5.84 |