Assay Detail
Binding
CHEMBL3225558
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Displacement of [3H]-pentazocine from human recombinant sigma-1 receptor expressed in CHO cells after 180 mins by beta counting analysis
20
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of novel selective Sigma-1 ligands as cognitive enhancers
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 7.01 | 8.50 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL408867 | [11C]SA4503 | — | 1 | 8.50 |
| CHEMBL3218986 | — | — | 1 | 8.00 |
| CHEMBL3218985 | — | — | 1 | 7.80 |
| CHEMBL3218989 | — | — | 1 | 7.60 |
| CHEMBL3218987 | — | — | 1 | 7.60 |
| CHEMBL3218982 | — | — | 1 | 7.20 |
| CHEMBL3218981 | — | — | 1 | 7.20 |
| CHEMBL3218992 | — | — | 1 | 7.10 |
| CHEMBL3218994 | — | — | 1 | 7.10 |
| CHEMBL3218993 | — | — | 1 | 7.00 |
| CHEMBL3218980 | — | — | 1 | 6.90 |
| CHEMBL98883 | — | — | 1 | 6.80 |
| CHEMBL3218979 | — | — | 3 | 6.80 |
| CHEMBL3218991 | — | — | 1 | 6.70 |
| CHEMBL3218984 | — | — | 1 | 6.40 |
| CHEMBL3218988 | — | — | 1 | 6.20 |
| CHEMBL3218983 | — | — | 1 | 5.90 |
| CHEMBL3218990 | — | — | 1 | 5.90 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL408867 | [11C]SA4503 | Ki | = | 3.162 | nM | 8.50 |
| CHEMBL3218986 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL3218985 | — | Ki | = | 15.85 | nM | 7.80 |
| CHEMBL3218989 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL3218987 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL3218982 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL3218981 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL3218994 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL3218992 | — | Ki | = | 79.43 | nM | 7.10 |
| CHEMBL3218993 | — | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL3218980 | — | Ki | = | 125.89 | nM | 6.90 |
| CHEMBL98883 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL3218979 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL3218979 | — | Ki | = | 158.49 | nM | 6.80 |
| CHEMBL3218979 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL3218991 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL3218984 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL3218988 | — | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL3218983 | — | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL3218990 | — | Ki | = | 1258.93 | nM | 5.90 |