Assay Detail
Binding
CHEMBL1104723
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
15
Total Activities
15
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
Conformationally constrained kappa receptor agonists: stereoselective synthesis and pharmacological evaluation of 6,8-diazabicyclo[3.2.2]nonane derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.08 | 8.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.41 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 8.38 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.21 |
| CHEMBL1096473 | — | — | 1 | 6.70 |
| CHEMBL1095520 | — | — | 1 | 6.36 |
| CHEMBL1096474 | — | — | 1 | 5.43 |
| CHEMBL1095184 | — | — | 1 | - |
| CHEMBL1094860 | — | — | 1 | - |
| CHEMBL1094237 | — | — | 1 | - |
| CHEMBL1094236 | — | — | 1 | - |
| CHEMBL1096475 | — | — | 1 | - |
| CHEMBL1095183 | — | — | 1 | - |
| CHEMBL1094880 | — | — | 1 | - |
| CHEMBL1096675 | — | — | 1 | - |
| CHEMBL1095521 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL1096473 | — | Ki | = | 198.0 | nM | 6.70 |
| CHEMBL1095520 | — | Ki | = | 433.0 | nM | 6.36 |
| CHEMBL1096474 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL1095184 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1094860 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1094237 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1094236 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1096475 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1095183 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1094880 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1096675 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL1095521 | — | Ki | > | 1000.0 | nM | - |