Assay Detail
Binding
CHEMBL4706007
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-DTG from sigma2 receptor in guinea pig brain membranes incubated for 120 mins by liquid scintillation counting method
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Tissue | Brain |
| Subcellular | Cell membrane |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
EST64454: a Highly Soluble σ Receptor Antagonist Clinical Candidate for Pain Management.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 18 | 7.01 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 7.66 |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | 7.64 |
| CHEMBL4792105 | — | — | 1 | 7.57 |
| CHEMBL4760287 | — | — | 1 | 7.55 |
| CHEMBL4795798 | — | — | 1 | 6.94 |
| CHEMBL4790686 | — | — | 1 | 6.86 |
| CHEMBL4759343 | — | — | 1 | 6.75 |
| CHEMBL4762627 | — | — | 1 | 6.63 |
| CHEMBL4792110 | — | — | 1 | 6.40 |
| CHEMBL60542 | (+)-PENTAZOCINE | — | 1 | 6.14 |
| CHEMBL2170062 | — | — | 1 | - |
| CHEMBL4786808 | — | — | 1 | - |
| CHEMBL4795269 | — | — | 1 | - |
| CHEMBL4782656 | — | — | 1 | - |
| CHEMBL4799271 | — | — | 1 | - |
| CHEMBL4757975 | — | — | 1 | - |
| CHEMBL4743610 | — | — | 1 | - |
| CHEMBL4776009 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4792105 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL4760287 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL4795798 | — | Ki | = | 116.0 | nM | 6.94 |
| CHEMBL4790686 | — | Ki | = | 137.0 | nM | 6.86 |
| CHEMBL4759343 | — | Ki | = | 180.0 | nM | 6.75 |
| CHEMBL4762627 | — | Ki | = | 232.0 | nM | 6.63 |
| CHEMBL4792110 | — | Ki | = | 399.0 | nM | 6.40 |
| CHEMBL60542 | (+)-PENTAZOCINE | Ki | = | 719.0 | nM | 6.14 |
| CHEMBL2170062 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4786808 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4795269 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4782656 | — | Ki | > | 1000.0 | nM | - |
| CHEMBL4799271 | — | Ki | - | — | - | |
| CHEMBL4757975 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4743610 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4776009 | — | Ki | > | 1000.0 | nM | - |