Assay Detail
Binding
CHEMBL753836
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity was determined in a crude membrane preparation from guinea pig brain by displacement of [3H]U-69593 from Opioid receptor kappa 1
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
(E)- and (Z)-7-arylidenenaltrexones: synthesis and opioid receptor radioligand displacement assays.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 11 | 7.17 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.96 |
| CHEMBL101519 | — | — | 1 | 7.47 |
| CHEMBL162267 | — | — | 1 | 7.43 |
| CHEMBL252172 | BNTX | — | 1 | 7.32 |
| CHEMBL164577 | — | — | 1 | 7.13 |
| CHEMBL350601 | — | — | 1 | 7.00 |
| CHEMBL434867 | — | — | 1 | 6.92 |
| CHEMBL349940 | — | — | 1 | 6.77 |
| CHEMBL165410 | — | — | 1 | 6.75 |
| CHEMBL355188 | — | — | 1 | 6.72 |
| CHEMBL162048 | — | — | 1 | 6.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL101519 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL162267 | — | Ki | = | 37.0 | nM | 7.43 |
| CHEMBL252172 | BNTX | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL164577 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL350601 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL434867 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL349940 | — | Ki | = | 170.0 | nM | 6.77 |
| CHEMBL165410 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL355188 | — | Ki | = | 190.0 | nM | 6.72 |
| CHEMBL162048 | — | Ki | = | 400.0 | nM | 6.40 |