Assay Detail
Binding
CHEMBL4396286
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-di-o-tolylguanidine from sigma2 receptor in rat liver membranes incubated for 120 mins by scintillation counting method
23
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membranes |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma intracellular receptor 2 (CHEMBL4105864) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Tetrahydro-3-benzazepines with fluorinated side chains as NMDA and σ<sub>1</sub> receptor antagonists: Synthesis, receptor affinity, selectivity and antiallodynic activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 6.68 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4588347 | — | — | 1 | 7.92 |
| CHEMBL4440895 | — | — | 3 | 7.41 |
| CHEMBL4575948 | — | — | 1 | 7.32 |
| CHEMBL4565798 | — | — | 1 | 7.25 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.24 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.11 |
| CHEMBL49623 | (R,S)-IFENPRODIL | — | 1 | 7.01 |
| CHEMBL4457961 | — | — | 1 | 6.94 |
| CHEMBL4514409 | — | — | 1 | 6.89 |
| CHEMBL4459710 | — | — | 1 | 6.82 |
| CHEMBL4536158 | — | — | 1 | 6.48 |
| CHEMBL4466227 | — | — | 1 | 6.28 |
| CHEMBL4435229 | — | — | 1 | 6.19 |
| CHEMBL4457995 | — | — | 1 | 6.13 |
| CHEMBL4562406 | — | — | 1 | 5.85 |
| CHEMBL4573419 | — | — | 1 | 5.75 |
| CHEMBL4473837 | — | — | 1 | 5.35 |
| CHEMBL4574220 | — | — | 1 | 5.10 |
| CHEMBL28564 | ELIPRODIL | 2.0 | 1 | - |
| CHEMBL1165411 | DEXOXADROL | 2.0 | 1 | - |
| CHEMBL284237 | DIZOCILPINE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4588347 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL4440895 | — | Ki | = | 39.0 | nM | 7.41 |
| CHEMBL4575948 | — | Ki | = | 48.0 | nM | 7.32 |
| CHEMBL4440895 | — | Ki | = | 49.0 | nM | 7.31 |
| CHEMBL4565798 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL4440895 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL49623 | (R,S)-IFENPRODIL | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4457961 | — | Ki | = | 115.0 | nM | 6.94 |
| CHEMBL4514409 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL4459710 | — | Ki | = | 153.0 | nM | 6.82 |
| CHEMBL4536158 | — | Ki | = | 333.0 | nM | 6.48 |
| CHEMBL4466227 | — | Ki | = | 524.0 | nM | 6.28 |
| CHEMBL4435229 | — | Ki | = | 643.0 | nM | 6.19 |
| CHEMBL4457995 | — | Ki | = | 740.0 | nM | 6.13 |
| CHEMBL4562406 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL4573419 | — | Ki | = | 1800.0 | nM | 5.75 |
| CHEMBL4473837 | — | Ki | = | 4500.0 | nM | 5.35 |
| CHEMBL4574220 | — | Ki | = | 7900.0 | nM | 5.10 |
| CHEMBL28564 | ELIPRODIL | Ki | - | — | - | |
| CHEMBL1165411 | DEXOXADROL | Ki | - | — | - | |
| CHEMBL284237 | DIZOCILPINE | Ki | - | — | - |