Assay Detail
Binding
CHEMBL4390736
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Displacement [3H]-DTG from sigma 2 receptor (unknown origin) expressed in HEK cell membranes
42
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 |
Publication
SYA 013 analogs as moderately selective sigma-2 (σ2) ligands: Structure-affinity relationship studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 42 | 7.81 | 8.67 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3321792 | — | — | 2 | 8.67 |
| CHEMBL4577233 | — | — | 2 | 8.66 |
| CHEMBL4446729 | — | — | 2 | 8.60 |
| CHEMBL476108 | — | — | 2 | 8.29 |
| CHEMBL1940412 | — | — | 1 | 8.29 |
| CHEMBL1946126 | — | — | 2 | 8.23 |
| CHEMBL4574793 | — | — | 2 | 8.10 |
| CHEMBL3321791 | — | — | 2 | 8.09 |
| CHEMBL4573441 | — | — | 2 | 8.08 |
| CHEMBL1946253 | — | — | 2 | 8.07 |
| CHEMBL4581305 | — | — | 1 | 7.88 |
| CHEMBL3321789 | — | — | 2 | 7.75 |
| CHEMBL3321788 | — | — | 2 | 7.60 |
| CHEMBL4554850 | — | — | 2 | 7.60 |
| CHEMBL1940414 | — | — | 1 | 7.60 |
| CHEMBL3321790 | — | — | 2 | 7.54 |
| CHEMBL4533305 | — | — | 2 | 7.50 |
| CHEMBL1940413 | — | — | 2 | 7.48 |
| CHEMBL4516724 | — | — | 2 | 7.40 |
| CHEMBL4462108 | — | — | 2 | 7.37 |
| CHEMBL340211 | AZAPERONE | 2.0 | 2 | 7.30 |
| CHEMBL1940408 | — | — | 1 | 7.29 |
| CHEMBL3289383 | — | — | 2 | 6.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3321792 | — | Ki | = | 2.138 | nM | 8.67 |
| CHEMBL3321792 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL4577233 | — | Ki | = | 2.2 | nM | 8.66 |
| CHEMBL4577233 | — | Ki | = | 2.239 | nM | 8.65 |
| CHEMBL4446729 | — | Ki | = | 2.512 | nM | 8.60 |
| CHEMBL4446729 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL476108 | — | Ki | = | 5.129 | nM | 8.29 |
| CHEMBL1940412 | — | Ki | = | 5.12 | nM | 8.29 |
| CHEMBL476108 | — | Ki | = | 5.6 | nM | 8.25 |
| CHEMBL1946126 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL1946126 | — | Ki | = | 5.888 | nM | 8.23 |
| CHEMBL4574793 | — | Ki | = | 7.943 | nM | 8.10 |
| CHEMBL4574793 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL3321791 | — | Ki | = | 8.1 | nM | 8.09 |
| CHEMBL3321791 | — | Ki | = | 8.128 | nM | 8.09 |
| CHEMBL4573441 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL4573441 | — | Ki | = | 8.511 | nM | 8.07 |
| CHEMBL1946253 | — | Ki | = | 8.511 | nM | 8.07 |
| CHEMBL1946253 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL4581305 | — | Ki | = | 13.1 | nM | 7.88 |
| CHEMBL3321789 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL3321789 | — | Ki | = | 19.95 | nM | 7.70 |
| CHEMBL3321788 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL4554850 | — | Ki | = | 25.12 | nM | 7.60 |
| CHEMBL1940414 | — | Ki | = | 25.1 | nM | 7.60 |
| CHEMBL4554850 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL3321788 | — | Ki | = | 27.0 | nM | 7.57 |
| CHEMBL3321790 | — | Ki | = | 29.0 | nM | 7.54 |
| CHEMBL3321790 | — | Ki | = | 29.51 | nM | 7.53 |
| CHEMBL4533305 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL4533305 | — | Ki | = | 32.36 | nM | 7.49 |
| CHEMBL1940413 | — | Ki | = | 33.11 | nM | 7.48 |
| CHEMBL1940413 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL4516724 | — | Ki | = | 39.81 | nM | 7.40 |
| CHEMBL4462108 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL4462108 | — | Ki | = | 42.66 | nM | 7.37 |
| CHEMBL4516724 | — | Ki | = | 44.0 | nM | 7.36 |
| CHEMBL340211 | AZAPERONE | Ki | = | 50.12 | nM | 7.30 |
| CHEMBL1940408 | — | Ki | = | 51.5 | nM | 7.29 |
| CHEMBL340211 | AZAPERONE | Ki | = | 52.0 | nM | 7.28 |
| CHEMBL3289383 | — | Ki | = | 600.0 | nM | 6.22 |
| CHEMBL3289383 | — | Ki | = | 630.96 | nM | 6.20 |