Assay Detail
Binding
CHEMBL751580
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Binding affinity determined against Opioid receptor mu 1 from human cloned receptor
12
Total Activities
12
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 | 12 | 7.96 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2111838 | — | — | 1 | 8.82 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 8.52 |
| CHEMBL127828 | — | — | 1 | 8.52 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 8.14 |
| CHEMBL2111836 | — | — | 1 | 8.04 |
| CHEMBL127969 | — | — | 1 | 8.03 |
| CHEMBL2448130 | — | — | 1 | 7.61 |
| CHEMBL124015 | — | — | 1 | 7.58 |
| CHEMBL2111837 | — | — | 1 | 7.56 |
| CHEMBL2448129 | — | — | 1 | 7.48 |
| CHEMBL2448128 | — | — | 1 | 7.26 |
| CHEMBL440765 | U-69593 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2111838 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL70 | MORPHINE | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL127828 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL2111836 | — | Ki | = | 9.2 | nM | 8.04 |
| CHEMBL127969 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL2448130 | — | Ki | = | 24.8 | nM | 7.61 |
| CHEMBL124015 | — | Ki | = | 26.3 | nM | 7.58 |
| CHEMBL2111837 | — | Ki | = | 27.4 | nM | 7.56 |
| CHEMBL2448129 | — | Ki | = | 33.2 | nM | 7.48 |
| CHEMBL2448128 | — | Ki | = | 54.8 | nM | 7.26 |
| CHEMBL440765 | U-69593 | Ki | > | 1000.0 | nM | - |