Assay Detail
Binding
CHEMBL2189107
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Displacement of [3H]U69,593 from kappa opioid receptor in guinea pig ileum membranes after 2 hrs
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Ileum |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 13 | 7.70 | 8.95 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2181193 | — | — | 1 | 8.95 |
| CHEMBL2181191 | — | — | 1 | 7.96 |
| CHEMBL2181196 | — | — | 1 | 7.94 |
| CHEMBL2181197 | — | — | 1 | 7.84 |
| CHEMBL2181201 | — | — | 1 | 7.79 |
| CHEMBL2181200 | — | — | 1 | 7.68 |
| CHEMBL2181202 | — | — | 1 | 7.65 |
| CHEMBL2181198 | — | — | 1 | 7.25 |
| CHEMBL2181199 | — | — | 1 | 7.01 |
| CHEMBL1782140 | — | — | 1 | 6.93 |
| CHEMBL2181192 | — | — | 1 | - |
| CHEMBL2181194 | — | — | 1 | - |
| CHEMBL2181195 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2181193 | — | Ki | = | 1.12 | nM | 8.95 |
| CHEMBL2181191 | — | Ki | = | 11.1 | nM | 7.96 |
| CHEMBL2181196 | — | Ki | = | 11.5 | nM | 7.94 |
| CHEMBL2181197 | — | Ki | = | 14.4 | nM | 7.84 |
| CHEMBL2181201 | — | Ki | = | 16.2 | nM | 7.79 |
| CHEMBL2181200 | — | Ki | = | 20.9 | nM | 7.68 |
| CHEMBL2181202 | — | Ki | = | 22.3 | nM | 7.65 |
| CHEMBL2181198 | — | Ki | = | 56.1 | nM | 7.25 |
| CHEMBL2181199 | — | Ki | = | 98.5 | nM | 7.01 |
| CHEMBL1782140 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL2181192 | — | Ki | - | — | - | |
| CHEMBL2181194 | — | Ki | - | — | - | |
| CHEMBL2181195 | — | Ki | > | 10.0 | nM | - |