Assay Detail
Binding
CHEMBL5097442
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-1,3-di-O-tolylguanidine from human sigma 2 receptor/TMEM97 transfected in sigma 1 receptor knockout HEK293 cell membranes assessed as inhibition constant measured after 120 mins by liquid scintillation counting analysis
32
Total Activities
30
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 |
Publication
Tricyclic Triazoles as σ<sub>1</sub> Receptor Antagonists for Treating Pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 32 | 6.81 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5190165 | — | — | 2 | 7.64 |
| CHEMBL5209229 | — | — | 1 | 7.29 |
| CHEMBL5209007 | — | — | 1 | 6.90 |
| CHEMBL5202041 | — | — | 2 | 6.88 |
| CHEMBL5193492 | — | — | 1 | 6.38 |
| CHEMBL5191285 | — | — | 1 | - |
| CHEMBL5186915 | — | — | 1 | - |
| CHEMBL5185431 | — | — | 1 | - |
| CHEMBL5202456 | — | — | 1 | - |
| CHEMBL5195143 | — | — | 1 | - |
| CHEMBL5170363 | — | — | 1 | - |
| CHEMBL5176813 | — | — | 1 | - |
| CHEMBL5190505 | — | — | 1 | - |
| CHEMBL5195219 | — | — | 1 | - |
| CHEMBL5192561 | — | — | 1 | - |
| CHEMBL5188036 | — | — | 1 | - |
| CHEMBL5198408 | — | — | 1 | - |
| CHEMBL5195592 | — | — | 1 | - |
| CHEMBL5197005 | — | — | 1 | - |
| CHEMBL5175398 | — | — | 1 | - |
| CHEMBL5195738 | — | — | 1 | - |
| CHEMBL5182178 | — | — | 1 | - |
| CHEMBL5181214 | — | — | 1 | - |
| CHEMBL5178219 | — | — | 1 | - |
| CHEMBL5197187 | — | — | 1 | - |
| CHEMBL5176858 | — | — | 1 | - |
| CHEMBL5183830 | — | — | 1 | - |
| CHEMBL5193266 | — | — | 1 | - |
| CHEMBL5173652 | — | — | 1 | - |
| CHEMBL5177384 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5190165 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL5209229 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL5209007 | — | Ki | = | 126.0 | nM | 6.90 |
| CHEMBL5202041 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL5190165 | — | Ki | = | 422.0 | nM | 6.38 |
| CHEMBL5193492 | — | Ki | = | 420.0 | nM | 6.38 |
| CHEMBL5202041 | — | Ki | = | 667.0 | nM | 6.18 |
| CHEMBL5195738 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5195219 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5175398 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5177384 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5195592 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5191285 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5185431 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5202456 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5195143 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5170363 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5176813 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5190505 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5192561 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5181214 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5178219 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5197187 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5176858 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5183830 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5193266 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5173652 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5188036 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5198408 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5186915 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5197005 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL5182178 | — | Ki | > | 10000.0 | nM | - |