Assay Detail
Binding
CHEMBL753633
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Displacement of [3H]- diprenorphine from mu-W318A-receptor expressed in HEK 293 cells
5
Total Activities
4
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 | 9.08 | 9.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | — | 2 | 9.66 |
| CHEMBL485832 | GUANIDINONALTRINDOLE | — | 1 | 9.30 |
| CHEMBL19019 | NALTREXONE | 4.0 | 1 | 8.60 |
| CHEMBL399708 | SPIROINDANYLOXYMORPHONE | — | 1 | 8.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 0.22 | nM | 9.66 |
| CHEMBL573214 | NORBINALTORPHIMINE | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL485832 | GUANIDINONALTRINDOLE | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL19019 | NALTREXONE | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL399708 | SPIROINDANYLOXYMORPHONE | Ki | = | 3.9 | nM | 8.41 |