Assay Detail
Functional
CHEMBL896956
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human kappa opioid receptor expressed in CHO cells assessed as stimulation of [35S]GTP-gamma-S binding
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| 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 |
|---|---|---|---|
| EC50 | 21 | 7.38 | 8.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113311 | — | — | 1 | 8.75 |
| CHEMBL2113314 | — | — | 1 | 8.48 |
| CHEMBL2113305 | — | — | 1 | 8.45 |
| CHEMBL2113313 | — | — | 1 | 8.40 |
| CHEMBL2113308 | — | — | 1 | 8.13 |
| CHEMBL2113307 | — | — | 1 | 8.06 |
| CHEMBL2113306 | — | — | 1 | 8.01 |
| CHEMBL2113312 | — | — | 1 | 7.85 |
| CHEMBL2113303 | — | — | 1 | 7.38 |
| CHEMBL2113296 | — | — | 1 | 7.25 |
| CHEMBL2113295 | — | — | 1 | 7.13 |
| CHEMBL2113309 | — | — | 1 | 6.97 |
| CHEMBL2113294 | — | — | 1 | 6.88 |
| CHEMBL2113299 | — | — | 1 | 6.88 |
| CHEMBL2113301 | — | — | 1 | 6.80 |
| CHEMBL2113310 | — | — | 1 | 6.63 |
| CHEMBL2113300 | — | — | 1 | 6.54 |
| CHEMBL2113297 | — | — | 1 | 6.54 |
| CHEMBL70 | MORPHINE | 4.0 | 1 | 6.32 |
| CHEMBL2113302 | — | — | 1 | 6.17 |
| CHEMBL511142 | BUPRENORPHINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113311 | — | EC50 | = | 1.78 | nM | 8.75 |
| CHEMBL2113314 | — | EC50 | = | 3.33 | nM | 8.48 |
| CHEMBL2113305 | — | EC50 | = | 3.52 | nM | 8.45 |
| CHEMBL2113313 | — | EC50 | = | 3.95 | nM | 8.40 |
| CHEMBL2113308 | — | EC50 | = | 7.49 | nM | 8.13 |
| CHEMBL2113307 | — | EC50 | = | 8.62 | nM | 8.06 |
| CHEMBL2113306 | — | EC50 | = | 9.88 | nM | 8.01 |
| CHEMBL2113312 | — | EC50 | = | 14.2 | nM | 7.85 |
| CHEMBL2113303 | — | EC50 | = | 41.7 | nM | 7.38 |
| CHEMBL2113296 | — | EC50 | = | 56.7 | nM | 7.25 |
| CHEMBL2113295 | — | EC50 | = | 74.4 | nM | 7.13 |
| CHEMBL2113309 | — | EC50 | = | 106.0 | nM | 6.97 |
| CHEMBL2113294 | — | EC50 | = | 131.0 | nM | 6.88 |
| CHEMBL2113299 | — | EC50 | = | 133.0 | nM | 6.88 |
| CHEMBL2113301 | — | EC50 | = | 159.0 | nM | 6.80 |
| CHEMBL2113310 | — | EC50 | = | 233.0 | nM | 6.63 |
| CHEMBL2113300 | — | EC50 | = | 285.0 | nM | 6.54 |
| CHEMBL2113297 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL70 | MORPHINE | EC50 | = | 484.0 | nM | 6.32 |
| CHEMBL2113302 | — | EC50 | = | 680.0 | nM | 6.17 |
| CHEMBL511142 | BUPRENORPHINE | EC50 | > | 10000.0 | nM | - |