Assay Detail
Binding
CHEMBL755684
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Displacement of [3H]U-69593 from human recombinant Opioid receptor kappa 1 on CHO cell membranes.
17
Total Activities
17
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 |
|---|---|---|---|
| Ki | 17 | 7.55 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | — | 1 | 9.70 |
| CHEMBL440765 | U-69593 | — | 1 | 9.52 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 9.40 |
| CHEMBL2113378 | — | — | 1 | 8.11 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 8.00 |
| CHEMBL2113382 | — | — | 1 | 7.86 |
| CHEMBL2113373 | — | — | 1 | 7.61 |
| CHEMBL2113377 | — | — | 1 | 7.44 |
| CHEMBL2113383 | — | — | 1 | 7.20 |
| CHEMBL2113380 | — | — | 1 | 7.20 |
| CHEMBL2113379 | — | — | 1 | 6.83 |
| CHEMBL38874 | DAMGO | — | 1 | 6.52 |
| CHEMBL401093 | OXYMORPHINDOLE | — | 1 | 6.40 |
| CHEMBL2113376 | — | — | 1 | 6.40 |
| CHEMBL2113372 | — | — | 1 | 6.39 |
| CHEMBL2113381 | — | — | 1 | 6.14 |
| CHEMBL31421 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL440765 | U-69593 | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL19019 | NALTREXONE | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2113378 | — | Ki | = | 7.79 | nM | 8.11 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 10.1 | nM | 8.00 |
| CHEMBL2113382 | — | Ki | = | 13.8 | nM | 7.86 |
| CHEMBL2113373 | — | Ki | = | 24.5 | nM | 7.61 |
| CHEMBL2113377 | — | Ki | = | 36.1 | nM | 7.44 |
| CHEMBL2113383 | — | Ki | = | 63.8 | nM | 7.20 |
| CHEMBL2113380 | — | Ki | = | 63.3 | nM | 7.20 |
| CHEMBL2113379 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL38874 | DAMGO | Ki | = | 305.0 | nM | 6.52 |
| CHEMBL401093 | OXYMORPHINDOLE | Ki | = | 396.0 | nM | 6.40 |
| CHEMBL2113376 | — | Ki | = | 399.0 | nM | 6.40 |
| CHEMBL2113372 | — | Ki | = | 409.0 | nM | 6.39 |
| CHEMBL2113381 | — | Ki | = | 723.0 | nM | 6.14 |
| CHEMBL31421 | — | Ki | > | 10000.0 | nM | - |