Assay Detail
Binding
CHEMBL755694
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Binding affinity against opioid receptor kappa 1 from human cloned receptor
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
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 | 25 | 9.02 | 9.77 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2111838 | — | — | 1 | 9.77 |
| CHEMBL123898 | — | — | 1 | 9.60 |
| CHEMBL341056 | — | — | 1 | 9.55 |
| CHEMBL127463 | — | — | 1 | 9.52 |
| CHEMBL341529 | — | — | 1 | 9.44 |
| CHEMBL127828 | — | — | 1 | 9.43 |
| CHEMBL2111836 | — | — | 1 | 9.37 |
| CHEMBL126688 | — | — | 1 | 9.35 |
| CHEMBL338391 | — | — | 1 | 9.33 |
| CHEMBL334156 | — | — | 1 | 9.28 |
| CHEMBL127968 | — | — | 1 | 9.26 |
| CHEMBL127969 | — | — | 1 | 9.24 |
| CHEMBL2111837 | — | — | 1 | 9.16 |
| CHEMBL2448130 | — | — | 1 | 9.15 |
| CHEMBL124015 | — | — | 1 | 9.15 |
| CHEMBL2448129 | — | — | 1 | 9.10 |
| CHEMBL440765 | U-69593 | — | 1 | 8.96 |
| CHEMBL2448128 | — | — | 1 | 8.89 |
| CHEMBL340001 | — | — | 1 | 8.88 |
| CHEMBL126282 | — | — | 1 | 8.82 |
| CHEMBL126596 | — | — | 1 | 8.42 |
| CHEMBL338393 | — | — | 1 | 8.36 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 8.36 |
| CHEMBL127619 | — | — | 1 | 7.87 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2111838 | — | Ki | = | 0.17 | nM | 9.77 |
| CHEMBL123898 | — | Ki | = | 0.25 | nM | 9.60 |
| CHEMBL341056 | — | Ki | = | 0.28 | nM | 9.55 |
| CHEMBL127463 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL341529 | — | Ki | = | 0.36 | nM | 9.44 |
| CHEMBL127828 | — | Ki | = | 0.37 | nM | 9.43 |
| CHEMBL2111836 | — | Ki | = | 0.43 | nM | 9.37 |
| CHEMBL126688 | — | Ki | = | 0.45 | nM | 9.35 |
| CHEMBL338391 | — | Ki | = | 0.47 | nM | 9.33 |
| CHEMBL334156 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL127968 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL127969 | — | Ki | = | 0.58 | nM | 9.24 |
| CHEMBL2111837 | — | Ki | = | 0.69 | nM | 9.16 |
| CHEMBL2448130 | — | Ki | = | 0.71 | nM | 9.15 |
| CHEMBL124015 | — | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2448129 | — | Ki | = | 0.79 | nM | 9.10 |
| CHEMBL440765 | U-69593 | Ki | = | 1.11 | nM | 8.96 |
| CHEMBL2448128 | — | Ki | = | 1.28 | nM | 8.89 |
| CHEMBL340001 | — | Ki | = | 1.31 | nM | 8.88 |
| CHEMBL126282 | — | Ki | = | 1.52 | nM | 8.82 |
| CHEMBL126596 | — | Ki | = | 3.77 | nM | 8.42 |
| CHEMBL338393 | — | Ki | = | 4.34 | nM | 8.36 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL127619 | — | Ki | = | 13.6 | nM | 7.87 |
| CHEMBL70 | MORPHINE | Ki | = | 64.0 | nM | 7.19 |