Assay Detail
Binding
CHEMBL4392610
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-Pentazocine from sigma 1 receptor (unknown origin) expressed in HEK293T cell membranes
23
Total Activities
12
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
New analogs of SYA013 as sigma-2 ligands with anticancer activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 23 | 7.65 | 8.61 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | 4.0 | 2 | 8.61 |
| CHEMBL4556093 | — | — | 2 | 8.31 |
| CHEMBL4566049 | — | — | 2 | 8.29 |
| CHEMBL4558031 | — | — | 2 | 7.80 |
| CHEMBL4463587 | — | — | 2 | 7.68 |
| CHEMBL4529943 | — | — | 1 | 7.68 |
| CHEMBL4474014 | — | — | 2 | 7.66 |
| CHEMBL4446568 | — | — | 2 | 7.59 |
| CHEMBL4570411 | — | — | 2 | 7.36 |
| CHEMBL1946124 | — | — | 2 | 7.20 |
| CHEMBL4459921 | — | — | 2 | 7.11 |
| CHEMBL4467840 | — | — | 2 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.455 | nM | 8.61 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 2.46 | nM | 8.61 |
| CHEMBL4556093 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL4556093 | — | Ki | = | 5.012 | nM | 8.30 |
| CHEMBL4566049 | — | Ki | = | 5.129 | nM | 8.29 |
| CHEMBL4566049 | — | Ki | = | 5.1 | nM | 8.29 |
| CHEMBL4558031 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4558031 | — | Ki | = | 16.22 | nM | 7.79 |
| CHEMBL4463587 | — | Ki | = | 20.89 | nM | 7.68 |
| CHEMBL4529943 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4463587 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4474014 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL4474014 | — | Ki | = | 22.39 | nM | 7.65 |
| CHEMBL4446568 | — | Ki | = | 25.7 | nM | 7.59 |
| CHEMBL4446568 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL4570411 | — | Ki | = | 43.65 | nM | 7.36 |
| CHEMBL4570411 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL1946124 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL1946124 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL4459921 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL4459921 | — | Ki | = | 77.62 | nM | 7.11 |
| CHEMBL4467840 | — | Ki | = | 251.19 | nM | 6.60 |
| CHEMBL4467840 | — | Ki | = | 277.0 | nM | 6.56 |