Assay Detail
Binding
CHEMBL839646
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In vitro binding affinity for human kappa opioid receptor was determined by using [3H]diprenorphine as radioligand
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Amino acid conjugates as kappa opioid receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 7.69 | 10.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL38576 | ICI-199,441 | — | 1 | 10.37 |
| CHEMBL181941 | — | — | 1 | 9.08 |
| CHEMBL179627 | — | — | 1 | 8.70 |
| CHEMBL361199 | — | — | 1 | 8.44 |
| CHEMBL180598 | — | — | 1 | 8.34 |
| CHEMBL178359 | — | — | 1 | 8.17 |
| CHEMBL359543 | — | — | 1 | 7.79 |
| CHEMBL178101 | — | — | 1 | 7.70 |
| CHEMBL369720 | — | — | 1 | 7.32 |
| CHEMBL181663 | — | — | 1 | 7.08 |
| CHEMBL182106 | — | — | 1 | 7.00 |
| CHEMBL368250 | — | — | 1 | 6.86 |
| CHEMBL179064 | — | — | 1 | 6.82 |
| CHEMBL181509 | — | — | 1 | 6.75 |
| CHEMBL360736 | — | — | 1 | 6.59 |
| CHEMBL178581 | — | — | 1 | 6.07 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL38576 | ICI-199,441 | Ki | = | 0.043 | nM | 10.37 |
| CHEMBL181941 | — | Ki | = | 0.83 | nM | 9.08 |
| CHEMBL179627 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL361199 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL180598 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL178359 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL359543 | — | Ki | = | 16.3 | nM | 7.79 |
| CHEMBL178101 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL369720 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL181663 | — | Ki | = | 84.0 | nM | 7.08 |
| CHEMBL182106 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL368250 | — | Ki | = | 138.0 | nM | 6.86 |
| CHEMBL179064 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL181509 | — | Ki | = | 178.0 | nM | 6.75 |
| CHEMBL360736 | — | Ki | = | 258.0 | nM | 6.59 |
| CHEMBL178581 | — | Ki | = | 856.0 | nM | 6.07 |