Assay Detail
Binding
CHEMBL759287
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Binding affinity against Opioid receptor kappa 1 of guinea pig using [3H]U-65693 as radioligand
9
Total Activities
9
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 quantitative receptor docking simulations of 2-[(acylamino)ethyl]-1,4-benzodiazepines as novel tifluadom-like ligands with high affinity and selectivity for kappa-opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 8.31 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL127969 | — | — | 1 | 9.30 |
| CHEMBL127463 | — | — | 1 | 9.25 |
| CHEMBL169703 | TIFLUADOM | 2.0 | 1 | 9.11 |
| CHEMBL341529 | — | — | 1 | 8.99 |
| CHEMBL127968 | — | — | 1 | 8.32 |
| CHEMBL124015 | — | — | 1 | 8.05 |
| CHEMBL126282 | — | — | 1 | 7.75 |
| CHEMBL340001 | — | — | 1 | 7.46 |
| CHEMBL127619 | — | — | 1 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL127969 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL127463 | — | Ki | = | 0.56 | nM | 9.25 |
| CHEMBL169703 | TIFLUADOM | Ki | = | 0.78 | nM | 9.11 |
| CHEMBL341529 | — | Ki | = | 1.03 | nM | 8.99 |
| CHEMBL127968 | — | Ki | = | 4.74 | nM | 8.32 |
| CHEMBL124015 | — | Ki | = | 8.84 | nM | 8.05 |
| CHEMBL126282 | — | Ki | = | 17.9 | nM | 7.75 |
| CHEMBL340001 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL127619 | — | Ki | = | 296.0 | nM | 6.53 |