Assay Detail
Binding
CHEMBL3379229
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]U-69593 from kappa opioid receptor in guinea pig brain membranes after 2 hrs by scintillation counting analysis
28
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 28 | 8.07 | 9.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1094879 | — | — | 1 | 9.51 |
| CHEMBL290543 | — | — | 1 | 9.47 |
| CHEMBL440765 | U-69593 | — | 1 | 9.01 |
| CHEMBL3323509 | — | — | 1 | 8.68 |
| CHEMBL3323511 | — | — | 1 | 8.57 |
| CHEMBL3323510 | — | — | 3 | 8.55 |
| CHEMBL3323513 | — | — | 1 | 8.51 |
| CHEMBL3323515 | — | — | 1 | 8.38 |
| CHEMBL3323516 | — | — | 1 | 8.37 |
| CHEMBL3323512 | — | — | 1 | 8.27 |
| CHEMBL3323508 | — | — | 1 | 8.18 |
| CHEMBL3323514 | — | — | 1 | 8.17 |
| CHEMBL80 | NALOXONE | 4.0 | 1 | 8.14 |
| CHEMBL3299002 | — | — | 1 | 8.03 |
| CHEMBL3299005 | — | — | 1 | 8.01 |
| CHEMBL3323522 | — | — | 1 | 7.96 |
| CHEMBL3323526 | — | — | 1 | 7.96 |
| CHEMBL3323523 | — | — | 1 | 7.82 |
| CHEMBL3323518 | — | — | 1 | 7.82 |
| CHEMBL3323527 | — | — | 1 | 7.75 |
| CHEMBL3323519 | — | — | 1 | 7.66 |
| CHEMBL3323520 | — | — | 1 | 7.62 |
| CHEMBL3323521 | — | — | 1 | 7.58 |
| CHEMBL3321775 | — | — | 1 | 6.87 |
| CHEMBL3323524 | — | — | 1 | 6.77 |
| CHEMBL3323525 | — | — | 1 | 6.32 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1094879 | — | Ki | = | 0.31 | nM | 9.51 |
| CHEMBL290543 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL440765 | U-69593 | Ki | = | 0.97 | nM | 9.01 |
| CHEMBL3323509 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3323511 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL3323510 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL3323513 | — | Ki | = | 3.1 | nM | 8.51 |
| CHEMBL3323515 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL3323516 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL3323512 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL3323508 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL3323514 | — | Ki | = | 6.8 | nM | 8.17 |
| CHEMBL80 | NALOXONE | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL3323510 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL3299002 | — | Ki | = | 9.4 | nM | 8.03 |
| CHEMBL3299005 | — | Ki | = | 9.7 | nM | 8.01 |
| CHEMBL3323522 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3323526 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL3323523 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3323518 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL3323510 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL3323527 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL3323519 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3323520 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL3323521 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL3321775 | — | Ki | = | 136.0 | nM | 6.87 |
| CHEMBL3323524 | — | Ki | = | 169.0 | nM | 6.77 |
| CHEMBL3323525 | — | Ki | = | 482.0 | nM | 6.32 |