Assay Detail
Binding
CHEMBL896953
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Displacement of [3H]U-69593 from human cloned kappa opioid receptor
25
Total Activities
25
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
Cinnamoyl derivatives of 7alpha-aminomethyl-6,14-endo-ethanotetrahydrothebaine and 7alpha-aminomethyl-6,14-endo-ethanotetrahydrooripavine and related opioid ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 8.06 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.40 |
| CHEMBL2113313 | — | — | 1 | 9.28 |
| CHEMBL2113666 | — | — | 1 | 9.27 |
| CHEMBL511142 | BUPRENORPHINE | 4.0 | 1 | 9.10 |
| CHEMBL2113314 | — | — | 1 | 8.85 |
| CHEMBL2113305 | — | — | 1 | 8.79 |
| CHEMBL2113308 | — | — | 1 | 8.76 |
| CHEMBL2113304 | — | — | 1 | 8.74 |
| CHEMBL2113307 | — | — | 1 | 8.73 |
| CHEMBL2113306 | — | — | 1 | 8.51 |
| CHEMBL2113303 | — | — | 1 | 8.28 |
| CHEMBL2113311 | — | — | 1 | 8.18 |
| CHEMBL2113312 | — | — | 1 | 8.00 |
| CHEMBL2113295 | — | — | 1 | 7.68 |
| CHEMBL2113296 | — | — | 1 | 7.65 |
| CHEMBL2113294 | — | — | 1 | 7.62 |
| CHEMBL2113309 | — | — | 1 | 7.58 |
| CHEMBL2113300 | — | — | 1 | 7.53 |
| CHEMBL2113301 | — | — | 1 | 7.35 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 7.33 |
| CHEMBL2113299 | — | — | 1 | 7.24 |
| CHEMBL2113310 | — | — | 1 | 7.17 |
| CHEMBL2113302 | — | — | 1 | 6.96 |
| CHEMBL2113298 | — | — | 1 | 6.81 |
| CHEMBL2113297 | — | — | 1 | 6.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL19019 | NALTREXONE | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2113313 | — | Ki | = | 0.52 | nM | 9.28 |
| CHEMBL2113666 | — | Ki | = | 0.54 | nM | 9.27 |
| CHEMBL511142 | BUPRENORPHINE | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2113314 | — | Ki | = | 1.41 | nM | 8.85 |
| CHEMBL2113305 | — | Ki | = | 1.64 | nM | 8.79 |
| CHEMBL2113308 | — | Ki | = | 1.72 | nM | 8.76 |
| CHEMBL2113304 | — | Ki | = | 1.82 | nM | 8.74 |
| CHEMBL2113307 | — | Ki | = | 1.85 | nM | 8.73 |
| CHEMBL2113306 | — | Ki | = | 3.11 | nM | 8.51 |
| CHEMBL2113303 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL2113311 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL2113312 | — | Ki | = | 9.95 | nM | 8.00 |
| CHEMBL2113295 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL2113296 | — | Ki | = | 22.2 | nM | 7.65 |
| CHEMBL2113294 | — | Ki | = | 23.7 | nM | 7.62 |
| CHEMBL2113309 | — | Ki | = | 26.4 | nM | 7.58 |
| CHEMBL2113300 | — | Ki | = | 29.8 | nM | 7.53 |
| CHEMBL2113301 | — | Ki | = | 44.7 | nM | 7.35 |
| CHEMBL70 | MORPHINE | Ki | = | 46.9 | nM | 7.33 |
| CHEMBL2113299 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL2113310 | — | Ki | = | 67.9 | nM | 7.17 |
| CHEMBL2113302 | — | Ki | = | 109.0 | nM | 6.96 |
| CHEMBL2113298 | — | Ki | = | 155.0 | nM | 6.81 |
| CHEMBL2113297 | — | Ki | = | 159.0 | nM | 6.80 |