Assay Detail
Binding
CHEMBL4033550
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-DTG from sigma2 receptor in guinea pig brain membrane after 120 mins by liquid scintillation counting method
19
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
(+)-Methyl (1R,2S)-2-{[4-(4-Chlorophenyl)-4-hydroxypiperidin-1-yl]methyl}-1-phenylcyclopropanecarboxylate [(+)-MR200] Derivatives as Potent and Selective Sigma Receptor Ligands: Stereochemistry and Pharmacological Properties.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 6.79 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.80 |
| CHEMBL4075591 | — | — | 3 | 7.66 |
| CHEMBL4070836 | — | — | 1 | 7.40 |
| CHEMBL4076606 | — | — | 1 | 7.24 |
| CHEMBL4061036 | — | — | 1 | 7.14 |
| CHEMBL4096913 | — | — | 1 | 6.97 |
| CHEMBL4079633 | — | — | 1 | 6.85 |
| CHEMBL4075797 | — | — | 1 | 6.84 |
| CHEMBL4091621 | — | — | 1 | 6.77 |
| CHEMBL4064312 | — | — | 1 | 6.68 |
| CHEMBL4075276 | — | — | 1 | 6.67 |
| CHEMBL4097493 | — | — | 1 | 6.54 |
| CHEMBL4069719 | — | — | 1 | 6.19 |
| CHEMBL4077113 | — | — | 1 | 6.04 |
| CHEMBL4081337 | — | — | 1 | 5.89 |
| CHEMBL4099359 | — | — | 1 | 5.79 |
| CHEMBL4076839 | — | — | 1 | 5.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4075591 | — | Ki | = | 21.9 | nM | 7.66 |
| CHEMBL4075591 | — | Ki | = | 23.4 | nM | 7.63 |
| CHEMBL4070836 | — | Ki | = | 40.0 | nM | 7.40 |
| CHEMBL4076606 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL4075591 | — | Ki | = | 61.1 | nM | 7.21 |
| CHEMBL4061036 | — | Ki | = | 73.0 | nM | 7.14 |
| CHEMBL4096913 | — | Ki | = | 107.0 | nM | 6.97 |
| CHEMBL4079633 | — | Ki | = | 142.0 | nM | 6.85 |
| CHEMBL4075797 | — | Ki | = | 146.0 | nM | 6.84 |
| CHEMBL4091621 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL4064312 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL4075276 | — | Ki | = | 214.0 | nM | 6.67 |
| CHEMBL4097493 | — | Ki | = | 290.0 | nM | 6.54 |
| CHEMBL4069719 | — | Ki | = | 650.0 | nM | 6.19 |
| CHEMBL4077113 | — | Ki | = | 918.0 | nM | 6.04 |
| CHEMBL4081337 | — | Ki | = | 1300.0 | nM | 5.89 |
| CHEMBL4099359 | — | Ki | = | 1638.0 | nM | 5.79 |
| CHEMBL4076839 | — | Ki | = | 1837.0 | nM | 5.74 |