Assay Detail
Binding
CHEMBL755490
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Displacement of [3H]diprenorphine from opioid receptor kappa 1 expressed in HEK 293 cells
5
Total Activities
5
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
Investigation of the selectivity of oxymorphone- and naltrexone-derived ligands via site-directed mutagenesis of opioid receptors: exploring the "address" recognition locus.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 5 | 7.74 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL485832 | GUANIDINONALTRINDOLE | — | 1 | 9.74 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.38 |
| CHEMBL567175 | NALTRINDOLE | — | 1 | 7.59 |
| CHEMBL963 | OXYMORPHONE | 4.0 | 1 | 6.68 |
| CHEMBL399708 | SPIROINDANYLOXYMORPHONE | — | 1 | 6.31 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL485832 | GUANIDINONALTRINDOLE | Ki | = | 0.18 | nM | 9.74 |
| CHEMBL19019 | NALTREXONE | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL567175 | NALTRINDOLE | Ki | = | 25.5 | nM | 7.59 |
| CHEMBL963 | OXYMORPHONE | Ki | = | 208.0 | nM | 6.68 |
| CHEMBL399708 | SPIROINDANYLOXYMORPHONE | Ki | = | 488.0 | nM | 6.31 |