Assay Detail
Binding
CHEMBL846101
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity for sigma 1 opioid receptor, measured on guinea pig brain membranes using [3H]- (+)-pentazocine as radioligand
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Membrane |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and structure-activity relationships of N-(1-benzylpiperidin-4-yl)arylacetamide analogues as potent sigma1 receptor ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 46 | 7.84 | 8.94 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL139340 | — | — | 1 | 8.94 |
| CHEMBL334568 | — | — | 1 | 8.92 |
| CHEMBL343752 | — | — | 1 | 8.75 |
| CHEMBL344425 | — | — | 1 | 8.65 |
| CHEMBL138794 | — | — | 1 | 8.64 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.60 |
| CHEMBL135083 | — | — | 1 | 8.50 |
| CHEMBL134855 | — | — | 1 | 8.49 |
| CHEMBL337796 | — | — | 1 | 8.46 |
| CHEMBL138688 | — | — | 1 | 8.41 |
| CHEMBL76895 | — | — | 1 | 8.41 |
| CHEMBL335953 | — | — | 1 | 8.40 |
| CHEMBL343580 | — | — | 1 | 8.38 |
| CHEMBL136114 | — | — | 1 | 8.37 |
| CHEMBL336037 | — | — | 1 | 8.33 |
| CHEMBL136451 | — | — | 1 | 8.26 |
| CHEMBL344023 | — | — | 1 | 8.20 |
| CHEMBL341957 | — | — | 1 | 8.18 |
| CHEMBL137675 | — | — | 1 | 8.17 |
| CHEMBL139156 | — | — | 1 | 8.14 |
| CHEMBL138249 | — | — | 1 | 8.14 |
| CHEMBL139629 | — | — | 1 | 8.09 |
| CHEMBL139735 | — | — | 1 | 8.04 |
| CHEMBL345051 | — | — | 1 | 7.99 |
| CHEMBL341936 | — | — | 1 | 7.96 |
| CHEMBL344402 | — | — | 1 | 7.86 |
| CHEMBL1036 | HYDROXYHALOPERIDOL | — | 1 | 7.84 |
| CHEMBL343137 | — | — | 1 | 7.81 |
| CHEMBL344186 | — | — | 1 | 7.72 |
| CHEMBL137041 | — | — | 1 | 7.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL139340 | — | Ki | = | 1.15 | nM | 8.94 |
| CHEMBL334568 | — | Ki | = | 1.21 | nM | 8.92 |
| CHEMBL343752 | — | Ki | = | 1.78 | nM | 8.75 |
| CHEMBL344425 | — | Ki | = | 2.25 | nM | 8.65 |
| CHEMBL138794 | — | Ki | = | 2.31 | nM | 8.64 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.53 | nM | 8.60 |
| CHEMBL135083 | — | Ki | = | 3.15 | nM | 8.50 |
| CHEMBL134855 | — | Ki | = | 3.21 | nM | 8.49 |
| CHEMBL337796 | — | Ki | = | 3.49 | nM | 8.46 |
| CHEMBL138688 | — | Ki | = | 3.93 | nM | 8.41 |
| CHEMBL76895 | — | Ki | = | 3.9 | nM | 8.41 |
| CHEMBL335953 | — | Ki | = | 3.97 | nM | 8.40 |
| CHEMBL343580 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL136114 | — | Ki | = | 4.29 | nM | 8.37 |
| CHEMBL336037 | — | Ki | = | 4.64 | nM | 8.33 |
| CHEMBL136451 | — | Ki | = | 5.51 | nM | 8.26 |
| CHEMBL344023 | — | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL341957 | — | Ki | = | 6.59 | nM | 8.18 |
| CHEMBL137675 | — | Ki | = | 6.75 | nM | 8.17 |
| CHEMBL139156 | — | Ki | = | 7.24 | nM | 8.14 |
| CHEMBL138249 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL139629 | — | Ki | = | 8.22 | nM | 8.09 |
| CHEMBL139735 | — | Ki | = | 9.03 | nM | 8.04 |
| CHEMBL345051 | — | Ki | = | 10.16 | nM | 7.99 |
| CHEMBL341936 | — | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL344402 | — | Ki | = | 13.82 | nM | 7.86 |
| CHEMBL1036 | HYDROXYHALOPERIDOL | Ki | = | 14.34 | nM | 7.84 |
| CHEMBL343137 | — | Ki | = | 15.41 | nM | 7.81 |
| CHEMBL344186 | — | Ki | = | 19.07 | nM | 7.72 |
| CHEMBL137041 | — | Ki | = | 22.66 | nM | 7.64 |
| CHEMBL136677 | — | Ki | = | 23.88 | nM | 7.62 |
| CHEMBL136275 | — | Ki | = | 31.25 | nM | 7.50 |
| CHEMBL139922 | — | Ki | = | 51.94 | nM | 7.28 |
| CHEMBL134856 | — | Ki | = | 61.77 | nM | 7.21 |
| CHEMBL136231 | — | Ki | = | 87.05 | nM | 7.06 |
| CHEMBL442408 | — | Ki | = | 125.41 | nM | 6.90 |
| CHEMBL423917 | — | Ki | = | 141.36 | nM | 6.85 |
| CHEMBL344873 | — | Ki | = | 149.84 | nM | 6.82 |
| CHEMBL138894 | — | Ki | = | 235.5 | nM | 6.63 |
| CHEMBL138393 | — | Ki | = | 248.36 | nM | 6.61 |
| CHEMBL137606 | — | Ki | = | 269.15 | nM | 6.57 |
| CHEMBL136989 | — | Ki | = | 298.47 | nM | 6.53 |
| CHEMBL138932 | — | Ki | = | 298.56 | nM | 6.53 |
| CHEMBL343927 | — | Ki | = | 346.9 | nM | 6.46 |
| CHEMBL136163 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL341680 | — | Ki | > | 1000.0 | nM | - |