Assay Detail
Binding
CHEMBL755511
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Stimulation of U-69,593 binding at human recombinant Opioid receptor kappa 1 transfected into CHO cells.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
14-amino, 14-alkylamino, and 14-acylamino analogs of oxymorphindole. Differential effects on opioid receptor binding and functional profiles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 16 | 6.95 | 7.79 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2113382 | — | — | 1 | 7.79 |
| CHEMBL440765 | U-69593 | — | 1 | 7.58 |
| CHEMBL2113378 | — | — | 1 | 7.57 |
| CHEMBL2113381 | — | — | 1 | 7.25 |
| CHEMBL2113379 | — | — | 1 | 7.02 |
| CHEMBL2113380 | — | — | 1 | 7.01 |
| CHEMBL2113377 | — | — | 1 | 6.03 |
| CHEMBL38874 | DAMGO | — | 1 | 5.36 |
| CHEMBL2113383 | — | — | 1 | - |
| CHEMBL2113376 | — | — | 1 | - |
| CHEMBL2113372 | — | — | 1 | - |
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | - |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | - |
| CHEMBL31421 | — | — | 1 | - |
| CHEMBL2113373 | — | — | 1 | - |
| CHEMBL567175 | NALTRINDOLE | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2113382 | — | EC50 | = | 16.4 | nM | 7.79 |
| CHEMBL440765 | U-69593 | EC50 | = | 26.1 | nM | 7.58 |
| CHEMBL2113378 | — | EC50 | = | 27.2 | nM | 7.57 |
| CHEMBL2113381 | — | EC50 | = | 56.9 | nM | 7.25 |
| CHEMBL2113379 | — | EC50 | = | 96.2 | nM | 7.02 |
| CHEMBL2113380 | — | EC50 | = | 96.5 | nM | 7.01 |
| CHEMBL2113377 | — | EC50 | = | 936.0 | nM | 6.03 |
| CHEMBL38874 | DAMGO | EC50 | = | 4365.0 | nM | 5.36 |
| CHEMBL2113383 | — | EC50 | = | 98.4 | Ke nM-1 | - |
| CHEMBL2113376 | — | EC50 | = | 86.8 | Ke nM-1 | - |
| CHEMBL2113372 | — | EC50 | = | 57.3 | Ke nM-1 | - |
| CHEMBL573214 | NORBINALTORPHIMINE | EC50 | = | 0.039 | Ke nM-1 | - |
| CHEMBL19019 | NALTREXONE | EC50 | = | 1.86 | Ke nM-1 | - |
| CHEMBL31421 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL2113373 | — | EC50 | = | 9.5 | Ke nM-1 | - |
| CHEMBL567175 | NALTRINDOLE | EC50 | = | 4.95 | Ke nM-1 | - |