Assay Detail
Binding
CHEMBL4033549
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain membrane after 150 mins by liquid scintillation counting method
20
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
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 | 20 | 7.78 | 8.87 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4076606 | — | — | 1 | 8.87 |
| CHEMBL4075591 | — | — | 3 | 8.82 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.66 |
| CHEMBL4088272 | — | — | 1 | 8.37 |
| CHEMBL4076839 | — | — | 1 | 8.15 |
| CHEMBL4070836 | — | — | 1 | 7.96 |
| CHEMBL4061036 | — | — | 1 | 7.92 |
| CHEMBL4091621 | — | — | 1 | 7.89 |
| CHEMBL4075797 | — | — | 1 | 7.85 |
| CHEMBL4064312 | — | — | 1 | 7.70 |
| CHEMBL4097493 | — | — | 1 | 7.48 |
| CHEMBL4075276 | — | — | 1 | 7.37 |
| CHEMBL4077113 | — | — | 1 | 7.35 |
| CHEMBL4096913 | — | — | 1 | 7.35 |
| CHEMBL4081337 | — | — | 1 | 7.28 |
| CHEMBL4099359 | — | — | 1 | 7.17 |
| CHEMBL4079633 | — | — | 1 | 6.89 |
| CHEMBL4069719 | — | — | 1 | 6.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4076606 | — | Ki | = | 1.35 | nM | 8.87 |
| CHEMBL4075591 | — | Ki | = | 1.51 | nM | 8.82 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL4088272 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL4075591 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL4076839 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4070836 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4061036 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4091621 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL4075797 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL4075591 | — | Ki | = | 14.6 | nM | 7.84 |
| CHEMBL4064312 | — | Ki | = | 20.0 | nM | 7.70 |
| CHEMBL4097493 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4075276 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL4077113 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL4096913 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL4081337 | — | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL4099359 | — | Ki | = | 67.0 | nM | 7.17 |
| CHEMBL4079633 | — | Ki | = | 129.0 | nM | 6.89 |
| CHEMBL4069719 | — | Ki | = | 445.0 | nM | 6.35 |