Assay Detail
Binding
CHEMBL4732777
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]pentazocine from human sigma 1 receptor expressed in HEK293 cell membrane incubated for 2 hrs by liquid scintillation counting method
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Studies on the affinity of 6-[(n-(cyclo)aminoalkyl)oxy]-4H-chromen-4-ones for sigma 1/2 receptors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 25 | 6.83 | 8.45 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.45 |
| CHEMBL408867 | [11C]SA4503 | — | 1 | 8.42 |
| CHEMBL2170062 | — | — | 1 | 7.77 |
| CHEMBL4781384 | — | — | 1 | 7.71 |
| CHEMBL4754019 | — | — | 1 | 7.62 |
| CHEMBL4754186 | — | — | 1 | 7.57 |
| CHEMBL4778747 | — | — | 1 | 7.18 |
| CHEMBL4751000 | — | — | 1 | 7.08 |
| CHEMBL4778990 | — | — | 1 | 7.06 |
| CHEMBL4799641 | — | — | 1 | 6.98 |
| CHEMBL4783222 | — | — | 1 | 6.95 |
| CHEMBL4781625 | — | — | 1 | 6.87 |
| CHEMBL4780620 | — | — | 1 | 6.67 |
| CHEMBL4765193 | — | — | 1 | 6.66 |
| CHEMBL4780719 | — | — | 1 | 6.64 |
| CHEMBL4779372 | — | — | 1 | 6.61 |
| CHEMBL4776765 | — | — | 1 | 6.51 |
| CHEMBL4765152 | — | — | 1 | 6.30 |
| CHEMBL4779000 | — | — | 1 | 6.22 |
| CHEMBL4760964 | — | — | 1 | 6.09 |
| CHEMBL4789695 | — | — | 1 | 6.08 |
| CHEMBL4794779 | — | — | 1 | 5.91 |
| CHEMBL4778900 | — | — | 1 | 5.54 |
| CHEMBL4794757 | — | — | 1 | 4.92 |
| CHEMBL4750183 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 3.53 | nM | 8.45 |
| CHEMBL408867 | [11C]SA4503 | Ki | = | 3.77 | nM | 8.42 |
| CHEMBL2170062 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4781384 | — | Ki | = | 19.6 | nM | 7.71 |
| CHEMBL4754019 | — | Ki | = | 23.9 | nM | 7.62 |
| CHEMBL4754186 | — | Ki | = | 27.2 | nM | 7.57 |
| CHEMBL4778747 | — | Ki | = | 65.5 | nM | 7.18 |
| CHEMBL4751000 | — | Ki | = | 82.5 | nM | 7.08 |
| CHEMBL4778990 | — | Ki | = | 87.0 | nM | 7.06 |
| CHEMBL4799641 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL4783222 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL4781625 | — | Ki | = | 134.0 | nM | 6.87 |
| CHEMBL4780620 | — | Ki | = | 213.0 | nM | 6.67 |
| CHEMBL4765193 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL4780719 | — | Ki | = | 227.0 | nM | 6.64 |
| CHEMBL4779372 | — | Ki | = | 245.0 | nM | 6.61 |
| CHEMBL4776765 | — | Ki | = | 309.0 | nM | 6.51 |
| CHEMBL4765152 | — | Ki | = | 499.0 | nM | 6.30 |
| CHEMBL4779000 | — | Ki | = | 604.0 | nM | 6.22 |
| CHEMBL4760964 | — | Ki | = | 809.0 | nM | 6.09 |
| CHEMBL4789695 | — | Ki | = | 825.0 | nM | 6.08 |
| CHEMBL4794779 | — | Ki | = | 1220.0 | nM | 5.91 |
| CHEMBL4778900 | — | Ki | = | 2870.0 | nM | 5.54 |
| CHEMBL4794757 | — | Ki | = | 12100.0 | nM | 4.92 |
| CHEMBL4750183 | — | Ki | > | 10000.0 | nM | - |