Assay Detail
Binding
CHEMBL758178
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Binding affinity was determined in a crude membrane preparation from guinea pig brain by displacement of [3H]DPDPE from Opioid receptor delta 1
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 8.01 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL162267 | — | — | 1 | 9.15 |
| CHEMBL350601 | — | — | 1 | 8.62 |
| CHEMBL101519 | — | — | 1 | 8.43 |
| CHEMBL434867 | — | — | 1 | 8.34 |
| CHEMBL252172 | BNTX | — | 1 | 8.21 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 7.96 |
| CHEMBL165410 | — | — | 1 | 7.80 |
| CHEMBL349940 | — | — | 1 | 7.77 |
| CHEMBL164577 | — | — | 1 | 7.41 |
| CHEMBL162048 | — | — | 1 | 7.33 |
| CHEMBL355188 | — | — | 1 | 7.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL162267 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL350601 | — | Ki | = | 2.4 | nM | 8.62 |
| CHEMBL101519 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL434867 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL252172 | BNTX | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL19019 | NALTREXONE | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL165410 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL349940 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL164577 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL162048 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL355188 | — | Ki | = | 75.0 | nM | 7.12 |