Assay Detail
Binding
CHEMBL4390735
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement [3H]-Pentazocine from sigma 1 receptor (unknown origin) expressed in HEK cell membranes
39
Total Activities
23
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
SYA 013 analogs as moderately selective sigma-2 (σ2) ligands: Structure-affinity relationship studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 39 | 7.29 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1946126 | — | — | 2 | 8.54 |
| CHEMBL1946253 | — | — | 2 | 8.44 |
| CHEMBL4577233 | — | — | 2 | 8.14 |
| CHEMBL3321788 | — | — | 2 | 7.66 |
| CHEMBL476108 | — | — | 2 | 7.63 |
| CHEMBL4573441 | — | — | 2 | 7.61 |
| CHEMBL4574793 | — | — | 2 | 7.52 |
| CHEMBL1940408 | — | — | 1 | 7.44 |
| CHEMBL1940412 | — | — | 1 | 7.38 |
| CHEMBL1940413 | — | — | 1 | 7.29 |
| CHEMBL3321792 | — | — | 2 | 7.24 |
| CHEMBL4533305 | — | — | 2 | 7.20 |
| CHEMBL4516724 | — | — | 2 | 7.20 |
| CHEMBL4581305 | — | — | 1 | 7.16 |
| CHEMBL3321791 | — | — | 2 | 7.15 |
| CHEMBL1940414 | — | — | 1 | 7.11 |
| CHEMBL3321790 | — | — | 2 | 7.09 |
| CHEMBL4462108 | — | — | 2 | 7.02 |
| CHEMBL4446729 | — | — | 1 | 6.95 |
| CHEMBL4554850 | — | — | 1 | 6.83 |
| CHEMBL3321789 | — | — | 2 | 6.78 |
| CHEMBL340211 | AZAPERONE | 2.0 | 2 | 6.39 |
| CHEMBL3289383 | — | — | 2 | 5.94 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1946126 | — | Ki | = | 2.884 | nM | 8.54 |
| CHEMBL1946126 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL1946253 | — | Ki | = | 3.6 | nM | 8.44 |
| CHEMBL1946253 | — | Ki | = | 3.631 | nM | 8.44 |
| CHEMBL4577233 | — | Ki | = | 7.244 | nM | 8.14 |
| CHEMBL4577233 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL3321788 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3321788 | — | Ki | = | 21.88 | nM | 7.66 |
| CHEMBL476108 | — | Ki | = | 23.44 | nM | 7.63 |
| CHEMBL476108 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL4573441 | — | Ki | = | 24.55 | nM | 7.61 |
| CHEMBL4573441 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL4574793 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL4574793 | — | Ki | = | 30.2 | nM | 7.52 |
| CHEMBL1940408 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL1940412 | — | Ki | = | 41.5 | nM | 7.38 |
| CHEMBL1940413 | — | Ki | = | 51.7 | nM | 7.29 |
| CHEMBL3321792 | — | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL3321792 | — | Ki | = | 57.0 | nM | 7.24 |
| CHEMBL4516724 | — | Ki | = | 63.1 | nM | 7.20 |
| CHEMBL4533305 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL4516724 | — | Ki | = | 63.0 | nM | 7.20 |
| CHEMBL4581305 | — | Ki | = | 70.0 | nM | 7.16 |
| CHEMBL3321791 | — | Ki | = | 70.79 | nM | 7.15 |
| CHEMBL3321791 | — | Ki | = | 71.0 | nM | 7.15 |
| CHEMBL1940414 | — | Ki | = | 77.1 | nM | 7.11 |
| CHEMBL3321790 | — | Ki | = | 81.28 | nM | 7.09 |
| CHEMBL3321790 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL4462108 | — | Ki | = | 95.0 | nM | 7.02 |
| CHEMBL4462108 | — | Ki | = | 95.5 | nM | 7.02 |
| CHEMBL4446729 | — | Ki | = | 113.0 | nM | 6.95 |
| CHEMBL4554850 | — | Ki | = | 148.0 | nM | 6.83 |
| CHEMBL3321789 | — | Ki | = | 166.0 | nM | 6.78 |
| CHEMBL3321789 | — | Ki | = | 165.96 | nM | 6.78 |
| CHEMBL340211 | AZAPERONE | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL340211 | AZAPERONE | Ki | = | 403.0 | nM | 6.39 |
| CHEMBL4533305 | — | Ki | = | 457.09 | nM | 6.34 |
| CHEMBL3289383 | — | Ki | = | 1148.0 | nM | 5.94 |
| CHEMBL3289383 | — | Ki | = | 1148.15 | nM | 5.94 |