Assay Detail
Binding
CHEMBL846104
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Binding affinity for sigma 2 opioid receptor, measured on rat liver membranes using [3H]- DTG as radioligand in the presence of (+)-pentazocine
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 3 — Cell-line / Tissue |
| Curated By | Expert |
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 | 6.88 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL334568 | — | — | 1 | 8.22 |
| CHEMBL139340 | — | — | 1 | 8.03 |
| CHEMBL137041 | — | — | 1 | 7.60 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.54 |
| CHEMBL1036 | HYDROXYHALOPERIDOL | — | 1 | 7.54 |
| CHEMBL138794 | — | — | 1 | 7.52 |
| CHEMBL136451 | — | — | 1 | 7.51 |
| CHEMBL336037 | — | — | 1 | 7.40 |
| CHEMBL136114 | — | — | 1 | 7.30 |
| CHEMBL337796 | — | — | 1 | 7.23 |
| CHEMBL344402 | — | — | 1 | 7.21 |
| CHEMBL341957 | — | — | 1 | 7.08 |
| CHEMBL343752 | — | — | 1 | 7.04 |
| CHEMBL136275 | — | — | 1 | 6.97 |
| CHEMBL134856 | — | — | 1 | 6.95 |
| CHEMBL135083 | — | — | 1 | 6.86 |
| CHEMBL344425 | — | — | 1 | 6.78 |
| CHEMBL335953 | — | — | 1 | 6.77 |
| CHEMBL343137 | — | — | 1 | 6.74 |
| CHEMBL136677 | — | — | 1 | 6.72 |
| CHEMBL137675 | — | — | 1 | 6.72 |
| CHEMBL343580 | — | — | 1 | 6.63 |
| CHEMBL344023 | — | — | 1 | 6.63 |
| CHEMBL76895 | — | — | 1 | 6.62 |
| CHEMBL134855 | — | — | 1 | 6.59 |
| CHEMBL136231 | — | — | 1 | 6.52 |
| CHEMBL344186 | — | — | 1 | 6.50 |
| CHEMBL138249 | — | — | 1 | 6.47 |
| CHEMBL138688 | — | — | 1 | 6.41 |
| CHEMBL138932 | — | — | 1 | 6.38 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL334568 | — | Ki | = | 6.06 | nM | 8.22 |
| CHEMBL139340 | — | Ki | = | 9.38 | nM | 8.03 |
| CHEMBL137041 | — | Ki | = | 25.02 | nM | 7.60 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 28.52 | nM | 7.54 |
| CHEMBL1036 | HYDROXYHALOPERIDOL | Ki | = | 28.55 | nM | 7.54 |
| CHEMBL138794 | — | Ki | = | 30.34 | nM | 7.52 |
| CHEMBL136451 | — | Ki | = | 31.02 | nM | 7.51 |
| CHEMBL336037 | — | Ki | = | 39.44 | nM | 7.40 |
| CHEMBL136114 | — | Ki | = | 50.26 | nM | 7.30 |
| CHEMBL337796 | — | Ki | = | 59.32 | nM | 7.23 |
| CHEMBL344402 | — | Ki | = | 61.31 | nM | 7.21 |
| CHEMBL341957 | — | Ki | = | 82.89 | nM | 7.08 |
| CHEMBL343752 | — | Ki | = | 90.31 | nM | 7.04 |
| CHEMBL136275 | — | Ki | = | 106.87 | nM | 6.97 |
| CHEMBL134856 | — | Ki | = | 111.57 | nM | 6.95 |
| CHEMBL135083 | — | Ki | = | 139.51 | nM | 6.86 |
| CHEMBL344425 | — | Ki | = | 167.63 | nM | 6.78 |
| CHEMBL335953 | — | Ki | = | 171.4 | nM | 6.77 |
| CHEMBL343137 | — | Ki | = | 181.3 | nM | 6.74 |
| CHEMBL136677 | — | Ki | = | 189.47 | nM | 6.72 |
| CHEMBL137675 | — | Ki | = | 191.05 | nM | 6.72 |
| CHEMBL343580 | — | Ki | = | 232.53 | nM | 6.63 |
| CHEMBL344023 | — | Ki | = | 231.61 | nM | 6.63 |
| CHEMBL76895 | — | Ki | = | 240.0 | nM | 6.62 |
| CHEMBL134855 | — | Ki | = | 256.62 | nM | 6.59 |
| CHEMBL136231 | — | Ki | = | 300.41 | nM | 6.52 |
| CHEMBL344186 | — | Ki | = | 319.07 | nM | 6.50 |
| CHEMBL138249 | — | Ki | = | 336.74 | nM | 6.47 |
| CHEMBL138688 | — | Ki | = | 392.82 | nM | 6.41 |
| CHEMBL138932 | — | Ki | = | 416.41 | nM | 6.38 |
| CHEMBL139156 | — | Ki | = | 423.17 | nM | 6.37 |
| CHEMBL423917 | — | Ki | = | 513.16 | nM | 6.29 |
| CHEMBL343927 | — | Ki | = | 631.0 | nM | 6.20 |
| CHEMBL345051 | — | Ki | = | 682.7 | nM | 6.17 |
| CHEMBL139922 | — | Ki | = | 678.28 | nM | 6.17 |
| CHEMBL139735 | — | Ki | = | 693.54 | nM | 6.16 |
| CHEMBL138894 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL136163 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL344873 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL139629 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL137606 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL341680 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL341936 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL136989 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL138393 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL442408 | — | Ki | > | 1000.0 | nM | - |