Assay Detail
Binding
CHEMBL5116793
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Binding affinity to sigma 1 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 7.27 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.60 |
| CHEMBL100116 | PENTAZOCINE | 4.0 | 1 | 8.33 |
| CHEMBL5169420 | — | — | 1 | 7.92 |
| CHEMBL5201355 | — | — | 1 | 7.80 |
| CHEMBL5186843 | — | — | 1 | 6.98 |
| CHEMBL5182253 | — | — | 1 | 6.43 |
| CHEMBL5187029 | — | — | 1 | 6.24 |
| CHEMBL5207122 | — | — | 1 | 5.84 |
| CHEMBL5206034 | — | — | 1 | - |
| CHEMBL5201238 | — | — | 1 | - |
| CHEMBL282433 | DITOLYLGUANIDINE | — | 1 | - |
| CHEMBL38874 | DAMGO | — | 1 | - |
| CHEMBL567175 | NALTRINDOLE | — | 1 | - |
| CHEMBL290543 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.5 | nM | 8.60 |
| CHEMBL100116 | PENTAZOCINE | Ki | = | 4.7 | nM | 8.33 |
| CHEMBL5169420 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5201355 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL5186843 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL5182253 | — | Ki | = | 375.0 | nM | 6.43 |
| CHEMBL5187029 | — | Ki | = | 573.0 | nM | 6.24 |
| CHEMBL5207122 | — | Ki | = | 1445.0 | nM | 5.84 |
| CHEMBL5206034 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL5201238 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL282433 | DITOLYLGUANIDINE | Ki | - | — | - | |
| CHEMBL38874 | DAMGO | Ki | - | — | - | |
| CHEMBL567175 | NALTRINDOLE | Ki | - | — | - | |
| CHEMBL290543 | — | Ki | - | — | - |