Assay Detail
Binding
CHEMBL4045547
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Displacement of [3H]-di-o-tolylguanidine from sigma 2 receptor in rat liver membranes after 120 mins by scintillation counting analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Replacement of benzylic hydroxy group by vinyl or hydroxymethyl moiety at the 3-benzazepine scaffold retaining GluN2B affinity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.81 | 7.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1289626 | — | — | 1 | 7.24 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.24 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.11 |
| CHEMBL4075349 | — | — | 1 | 6.93 |
| CHEMBL1289403 | — | — | 1 | 6.26 |
| CHEMBL4088218 | — | — | 1 | 6.05 |
| CHEMBL4065052 | — | — | 1 | - |
| CHEMBL319706 | (S)-IFENPRODIL | — | 1 | - |
| CHEMBL1165411 | DEXOXADROL | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1289626 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4075349 | — | Ki | = | 118.0 | nM | 6.93 |
| CHEMBL1289403 | — | Ki | = | 554.0 | nM | 6.26 |
| CHEMBL4088218 | — | Ki | = | 883.0 | nM | 6.05 |
| CHEMBL4065052 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL319706 | (S)-IFENPRODIL | Ki | - | — | - | |
| CHEMBL1165411 | DEXOXADROL | Ki | - | — | - |