Assay Detail
Binding
CHEMBL934064
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Displacement of [3H]DTG from opioid sigma2 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 | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
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 | 8.42 | 9.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL270341 | — | — | 1 | 9.41 |
| CHEMBL272603 | — | — | 1 | 9.26 |
| CHEMBL272854 | — | — | 1 | 9.11 |
| CHEMBL53325 | — | — | 1 | 8.96 |
| CHEMBL272608 | — | — | 1 | 8.83 |
| CHEMBL271772 | — | — | 1 | 8.74 |
| CHEMBL271975 | — | — | 1 | 8.65 |
| CHEMBL406081 | — | — | 1 | 8.61 |
| CHEMBL273084 | — | — | 1 | 8.52 |
| CHEMBL272610 | — | — | 1 | 8.51 |
| CHEMBL408003 | — | — | 1 | 8.42 |
| CHEMBL269876 | — | — | 1 | 8.27 |
| CHEMBL406082 | — | — | 1 | 8.23 |
| CHEMBL405925 | — | — | 1 | 8.06 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.09 |
| CHEMBL272899 | — | — | 1 | 6.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL270341 | — | Ki | = | 0.39 | nM | 9.41 |
| CHEMBL272603 | — | Ki | = | 0.55 | nM | 9.26 |
| CHEMBL272854 | — | Ki | = | 0.77 | nM | 9.11 |
| CHEMBL53325 | — | Ki | = | 1.11 | nM | 8.96 |
| CHEMBL272608 | — | Ki | = | 1.49 | nM | 8.83 |
| CHEMBL271772 | — | Ki | = | 1.83 | nM | 8.74 |
| CHEMBL271975 | — | Ki | = | 2.25 | nM | 8.65 |
| CHEMBL406081 | — | Ki | = | 2.44 | nM | 8.61 |
| CHEMBL273084 | — | Ki | = | 3.05 | nM | 8.52 |
| CHEMBL272610 | — | Ki | = | 3.06 | nM | 8.51 |
| CHEMBL408003 | — | Ki | = | 3.77 | nM | 8.42 |
| CHEMBL269876 | — | Ki | = | 5.43 | nM | 8.27 |
| CHEMBL406082 | — | Ki | = | 5.89 | nM | 8.23 |
| CHEMBL405925 | — | Ki | = | 8.74 | nM | 8.06 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 80.6 | nM | 7.09 |
| CHEMBL272899 | — | Ki | = | 830.95 | nM | 6.08 |