Assay Detail
Binding
CHEMBL955071
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Displacement of [3H]U69,593 from human kappa opioid receptor expressed in CHO cells after 60 mins by scintillation counting
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Syntheses of novel high affinity ligands for opioid receptors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.55 | 9.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.72 |
| CHEMBL471243 | — | — | 1 | 9.64 |
| CHEMBL511816 | — | — | 1 | 9.62 |
| CHEMBL470005 | — | — | 1 | 9.54 |
| CHEMBL511645 | — | — | 1 | 9.47 |
| CHEMBL513762 | — | — | 1 | 9.34 |
| CHEMBL469815 | — | — | 1 | 9.09 |
| CHEMBL471048 | — | — | 1 | 8.64 |
| CHEMBL398707 | HYDROMORPHONE | 4.0 | 1 | 8.55 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 8.54 |
| CHEMBL895 | NALBUPHINE | 4.0 | 1 | 8.52 |
| CHEMBL470617 | NALTREXONE METHIODIDE | — | 1 | 8.20 |
| CHEMBL511302 | — | — | 1 | 8.11 |
| CHEMBL512150 | — | — | 1 | 8.05 |
| CHEMBL56695 | — | — | 1 | 7.96 |
| CHEMBL511621 | — | — | 1 | 7.80 |
| CHEMBL471049 | — | — | 1 | 7.72 |
| CHEMBL511795 | — | — | 1 | 7.33 |
| CHEMBL511461 | — | — | 1 | 6.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Ki | = | 0.19 | nM | 9.72 |
| CHEMBL471243 | — | Ki | = | 0.23 | nM | 9.64 |
| CHEMBL511816 | — | Ki | = | 0.24 | nM | 9.62 |
| CHEMBL470005 | — | Ki | = | 0.29 | nM | 9.54 |
| CHEMBL511645 | — | Ki | = | 0.34 | nM | 9.47 |
| CHEMBL513762 | — | Ki | = | 0.46 | nM | 9.34 |
| CHEMBL469815 | — | Ki | = | 0.81 | nM | 9.09 |
| CHEMBL471048 | — | Ki | = | 2.3 | nM | 8.64 |
| CHEMBL398707 | HYDROMORPHONE | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL895 | NALBUPHINE | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL470617 | NALTREXONE METHIODIDE | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL511302 | — | Ki | = | 7.7 | nM | 8.11 |
| CHEMBL512150 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL56695 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL511621 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL471049 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL511795 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL511461 | — | Ki | = | 210.0 | nM | 6.68 |