Assay Detail
Binding
CHEMBL754739
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity determined against Opioid receptor kappa 1 from a native receptor in guinea pig
19
Total Activities
19
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
Synthesis, biological evaluation, and receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as kappa-opioid receptor agonists endowed with antinociceptive and antiamnesic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.23 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2111836 | — | — | 1 | 9.72 |
| CHEMBL127969 | — | — | 1 | 9.30 |
| CHEMBL127463 | — | — | 1 | 9.25 |
| CHEMBL127828 | — | — | 1 | 9.11 |
| CHEMBL341529 | — | — | 1 | 8.99 |
| CHEMBL126688 | — | — | 1 | 8.76 |
| CHEMBL440765 | U-69593 | — | 1 | 8.72 |
| CHEMBL2448128 | — | — | 1 | 8.61 |
| CHEMBL2111837 | — | — | 1 | 8.35 |
| CHEMBL127968 | — | — | 1 | 8.32 |
| CHEMBL2448129 | — | — | 1 | 8.18 |
| CHEMBL124015 | — | — | 1 | 8.05 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 7.99 |
| CHEMBL126282 | — | — | 1 | 7.75 |
| CHEMBL338393 | — | — | 1 | 7.59 |
| CHEMBL340001 | — | — | 1 | 7.46 |
| CHEMBL126596 | — | — | 1 | 6.94 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.82 |
| CHEMBL127619 | — | — | 1 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2111836 | — | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL127969 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL127463 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL127828 | — | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL341529 | — | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL126688 | — | Ki | = | 1.74 | nM | 8.76 |
| CHEMBL440765 | U-69593 | Ki | = | 1.89 | nM | 8.72 |
| CHEMBL2448128 | — | Ki | = | 2.46 | nM | 8.61 |
| CHEMBL2111837 | — | Ki | = | 4.52 | nM | 8.35 |
| CHEMBL127968 | — | Ki | = | 4.74 | nM | 8.32 |
| CHEMBL2448129 | — | Ki | = | 6.55 | nM | 8.18 |
| CHEMBL124015 | — | Ki | = | 8.84 | nM | 8.05 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 10.2 | nM | 7.99 |
| CHEMBL126282 | — | Ki | = | 17.9 | nM | 7.75 |
| CHEMBL338393 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL340001 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL126596 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL70 | MORPHINE | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL127619 | — | Ki | = | 296.0 | nM | 6.53 |