Assay Detail
Binding
CHEMBL907786
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Displacement of [3H]U-69593 from human recombinant kappa opioid receptor expressed in CHO cells
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 | Expert |
Publication
Structural determinants of opioid activity in derivatives of 14-aminomorphinones: effects of changes to the chain linking of the C14-amino group to the aryl ring.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.16 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.40 |
| CHEMBL448428 | — | — | 1 | 9.00 |
| CHEMBL386492 | CLOCINNAMOX | — | 1 | 8.85 |
| CHEMBL217658 | — | — | 1 | 8.81 |
| CHEMBL277530 | — | — | 1 | 8.59 |
| CHEMBL217479 | — | — | 1 | 8.53 |
| CHEMBL383896 | — | — | 1 | 8.43 |
| CHEMBL216558 | — | — | 1 | 8.43 |
| CHEMBL217710 | — | — | 1 | 8.31 |
| CHEMBL217102 | — | — | 1 | 8.28 |
| CHEMBL263482 | — | — | 1 | 8.12 |
| CHEMBL387101 | — | — | 1 | 7.88 |
| CHEMBL386272 | — | — | 1 | 7.79 |
| CHEMBL216365 | — | — | 1 | 7.67 |
| CHEMBL217790 | — | — | 1 | 7.60 |
| CHEMBL384118 | — | — | 1 | 7.59 |
| CHEMBL411089 | — | — | 1 | 7.47 |
| CHEMBL215926 | — | — | 1 | 7.38 |
| CHEMBL387016 | — | — | 1 | 6.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL448428 | — | Ki | = | 1.0 | nM | 9.00 |
| CHEMBL386492 | CLOCINNAMOX | Ki | = | 1.41 | nM | 8.85 |
| CHEMBL217658 | — | Ki | = | 1.53 | nM | 8.81 |
| CHEMBL277530 | — | Ki | = | 2.59 | nM | 8.59 |
| CHEMBL217479 | — | Ki | = | 2.95 | nM | 8.53 |
| CHEMBL383896 | — | Ki | = | 3.69 | nM | 8.43 |
| CHEMBL216558 | — | Ki | = | 3.72 | nM | 8.43 |
| CHEMBL217710 | — | Ki | = | 4.94 | nM | 8.31 |
| CHEMBL217102 | — | Ki | = | 5.27 | nM | 8.28 |
| CHEMBL263482 | — | Ki | = | 7.51 | nM | 8.12 |
| CHEMBL387101 | — | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL386272 | — | Ki | = | 16.4 | nM | 7.79 |
| CHEMBL216365 | — | Ki | = | 21.5 | nM | 7.67 |
| CHEMBL217790 | — | Ki | = | 25.2 | nM | 7.60 |
| CHEMBL384118 | — | Ki | = | 25.9 | nM | 7.59 |
| CHEMBL411089 | — | Ki | = | 33.5 | nM | 7.47 |
| CHEMBL215926 | — | Ki | = | 41.5 | nM | 7.38 |
| CHEMBL387016 | — | Ki | = | 128.0 | nM | 6.89 |