Assay Detail
Binding
CHEMBL5097441
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from human sigma1 receptor transfected in HEK293 cell membranes assessed as inhibition constant measured after 120 mins by liquid scintillation counting analysis
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Tricyclic Triazoles as σ<sub>1</sub> Receptor Antagonists for Treating Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 36 | 7.43 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5186915 | — | — | 1 | 8.52 |
| CHEMBL5189328 | — | — | 1 | 8.22 |
| CHEMBL5197005 | — | — | 1 | 8.05 |
| CHEMBL5181214 | — | — | 1 | 7.96 |
| CHEMBL5209229 | — | — | 1 | 7.92 |
| CHEMBL5188036 | — | — | 1 | 7.85 |
| CHEMBL5193266 | — | — | 1 | 7.85 |
| CHEMBL5182348 | — | — | 1 | 7.80 |
| CHEMBL5173173 | — | — | 1 | 7.80 |
| CHEMBL5173652 | — | — | 1 | 7.80 |
| CHEMBL2170062 | — | — | 1 | 7.77 |
| CHEMBL5192561 | — | — | 1 | 7.68 |
| CHEMBL5197187 | — | — | 1 | 7.66 |
| CHEMBL5198408 | — | — | 1 | 7.60 |
| CHEMBL5209007 | — | — | 1 | 7.58 |
| CHEMBL5173523 | — | — | 1 | 7.57 |
| CHEMBL5193492 | — | — | 1 | 7.51 |
| CHEMBL5195143 | — | — | 1 | 7.31 |
| CHEMBL5195738 | — | — | 1 | 7.29 |
| CHEMBL5183830 | — | — | 1 | 7.20 |
| CHEMBL5185431 | — | — | 1 | 7.14 |
| CHEMBL5176813 | — | — | 1 | 7.13 |
| CHEMBL5190505 | — | — | 1 | 7.07 |
| CHEMBL5175398 | — | — | 1 | 7.06 |
| CHEMBL5170363 | — | — | 1 | 6.92 |
| CHEMBL5177384 | — | — | 1 | 6.91 |
| CHEMBL5178219 | — | — | 1 | 6.68 |
| CHEMBL5182178 | — | — | 1 | 6.41 |
| CHEMBL5191285 | — | — | 1 | 6.35 |
| CHEMBL5195219 | — | — | 1 | 6.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5186915 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL5189328 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL5197005 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL5181214 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL5209229 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5188036 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5193266 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL5182348 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL5173173 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL5173652 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2170062 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL5192561 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL5197187 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL5198408 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL5209007 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL5173523 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL5193492 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL5195143 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL5195738 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL5183830 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL5185431 | — | Ki | = | 72.0 | nM | 7.14 |
| CHEMBL5176813 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL5190505 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL5175398 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL5170363 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL5177384 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL5178219 | — | Ki | = | 209.0 | nM | 6.68 |
| CHEMBL5182178 | — | Ki | = | 392.0 | nM | 6.41 |
| CHEMBL5191285 | — | Ki | = | 446.0 | nM | 6.35 |
| CHEMBL5195219 | — | Ki | = | 611.0 | nM | 6.21 |
| CHEMBL5176858 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5195592 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5205938 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5191799 | — | Ki | > | 10.0 | nM | - |
| CHEMBL5202456 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5194191 | — | Ki | > | 1000.0 | nM | - |