Assay Detail
Binding
CHEMBL753682
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Binding affinity towards rat opioid receptor kappa 1 was determined using [3H]diprenorphine radioligand
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 4 | 8.65 | 9.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL485832 | GUANIDINONALTRINDOLE | — | 1 | 9.85 |
| CHEMBL610279 | — | — | 1 | 8.94 |
| CHEMBL610280 | — | — | 1 | 7.16 |
| CHEMBL610535 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL485832 | GUANIDINONALTRINDOLE | Ki | = | 0.14 | nM | 9.85 |
| CHEMBL610279 | — | Ki | = | 1.15 | nM | 8.94 |
| CHEMBL610280 | — | Ki | = | 69.1 | nM | 7.16 |
| CHEMBL610535 | — | Ki | > | 1000.0 | nM | - |