Assay Detail
Binding
CHEMBL4396285
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-(+)-pentazocine from sigma1 receptor in guinea pig brain cortex 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 | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL4153) ↗| Type | SINGLE PROTEIN |
| Organism | Cavia porcellus |
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 | 7.22 | 8.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.20 |
| CHEMBL4457961 | — | — | 1 | 8.18 |
| CHEMBL4575948 | — | — | 1 | 8.10 |
| CHEMBL4440895 | — | — | 3 | 8.00 |
| CHEMBL4565798 | — | — | 1 | 7.96 |
| CHEMBL4466227 | — | — | 1 | 7.60 |
| CHEMBL4588347 | — | — | 1 | 7.50 |
| CHEMBL4459710 | — | — | 1 | 7.16 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.05 |
| CHEMBL4536158 | — | — | 1 | 6.97 |
| CHEMBL49623 | (R,S)-IFENPRODIL | — | 1 | 6.90 |
| CHEMBL4573419 | — | — | 1 | 6.74 |
| CHEMBL4435229 | — | — | 1 | 6.73 |
| CHEMBL4473837 | — | — | 1 | 6.68 |
| CHEMBL4457995 | — | — | 1 | 6.67 |
| CHEMBL4562406 | — | — | 1 | 6.41 |
| CHEMBL4574220 | — | — | 1 | 6.23 |
| CHEMBL4514409 | — | — | 1 | 5.85 |
| CHEMBL28564 | ELIPRODIL | 2.0 | 1 | - |
| CHEMBL1165411 | DEXOXADROL | 2.0 | 1 | - |
| CHEMBL284237 | DIZOCILPINE | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 6.3 | nM | 8.20 |
| CHEMBL4457961 | — | Ki | = | 6.6 | nM | 8.18 |
| CHEMBL4575948 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4440895 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL4565798 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4440895 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4466227 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4440895 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4588347 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4459710 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 89.0 | nM | 7.05 |
| CHEMBL4536158 | — | Ki | = | 108.0 | nM | 6.97 |
| CHEMBL49623 | (R,S)-IFENPRODIL | Ki | = | 125.0 | nM | 6.90 |
| CHEMBL4573419 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL4435229 | — | Ki | = | 185.0 | nM | 6.73 |
| CHEMBL4473837 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL4457995 | — | Ki | = | 213.0 | nM | 6.67 |
| CHEMBL4562406 | — | Ki | = | 393.0 | nM | 6.41 |
| CHEMBL4574220 | — | Ki | = | 585.0 | nM | 6.23 |
| CHEMBL4514409 | — | Ki | = | 1400.0 | nM | 5.85 |
| CHEMBL28564 | ELIPRODIL | Ki | - | — | - | |
| CHEMBL1165411 | DEXOXADROL | Ki | - | — | - | |
| CHEMBL284237 | DIZOCILPINE | Ki | - | — | - |