Assay Detail
Binding
CHEMBL755494
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Effect on binding to wild-type opioid receptor kappa 1 using [3H]diprenorphine in transiently expressed rat HEK293 cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HEK293 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Transformation of a kappa-opioid receptor antagonist to a kappa-agonist by transfer of a guanidinium group from the 5'- to 6'-position of naltrindole.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 3 | 8.71 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL485832 | GUANIDINONALTRINDOLE | — | 1 | 9.68 |
| CHEMBL610279 | — | — | 1 | 8.95 |
| CHEMBL610280 | — | — | 1 | 7.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL485832 | GUANIDINONALTRINDOLE | Ki | = | 0.21 | nM | 9.68 |
| CHEMBL610279 | — | Ki | = | 1.13 | nM | 8.95 |
| CHEMBL610280 | — | Ki | = | 32.7 | nM | 7.49 |