Assay Detail
Binding
CHEMBL934063
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H](+)-pentazocine from opioid sigma1 receptor in rat brain homogenate
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Brain |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Conversion of a highly selective sigma-1 receptor-ligand to sigma-2 receptor preferring ligands with anticocaine activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 16 | 8.44 | 9.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL272899 | — | — | 1 | 9.92 |
| CHEMBL272603 | — | — | 1 | 8.89 |
| CHEMBL53325 | — | — | 1 | 8.83 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.47 |
| CHEMBL408003 | — | — | 1 | 8.47 |
| CHEMBL270341 | — | — | 1 | 8.38 |
| CHEMBL272610 | — | — | 1 | 8.34 |
| CHEMBL271975 | — | — | 1 | 8.33 |
| CHEMBL272854 | — | — | 1 | 8.31 |
| CHEMBL406081 | — | — | 1 | 8.30 |
| CHEMBL405925 | — | — | 1 | 8.28 |
| CHEMBL273084 | — | — | 1 | 8.25 |
| CHEMBL272608 | — | — | 1 | 8.18 |
| CHEMBL269876 | — | — | 1 | 8.16 |
| CHEMBL406082 | — | — | 1 | 7.98 |
| CHEMBL271772 | — | — | 1 | 7.95 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL272899 | — | Ki | = | 0.12 | nM | 9.92 |
| CHEMBL272603 | — | Ki | = | 1.28 | nM | 8.89 |
| CHEMBL53325 | — | Ki | = | 1.48 | nM | 8.83 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 3.35 | nM | 8.47 |
| CHEMBL408003 | — | Ki | = | 3.37 | nM | 8.47 |
| CHEMBL270341 | — | Ki | = | 4.17 | nM | 8.38 |
| CHEMBL272610 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL271975 | — | Ki | = | 4.66 | nM | 8.33 |
| CHEMBL272854 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL406081 | — | Ki | = | 4.98 | nM | 8.30 |
| CHEMBL405925 | — | Ki | = | 5.22 | nM | 8.28 |
| CHEMBL273084 | — | Ki | = | 5.61 | nM | 8.25 |
| CHEMBL272608 | — | Ki | = | 6.55 | nM | 8.18 |
| CHEMBL269876 | — | Ki | = | 6.9 | nM | 8.16 |
| CHEMBL406082 | — | Ki | = | 10.55 | nM | 7.98 |
| CHEMBL271772 | — | Ki | = | 11.26 | nM | 7.95 |