Assay Detail
Binding
CHEMBL803930
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In vitro binding affinity towards sigma receptor by the displacement of [3H]PPP from guinea pig brain
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL287) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and evaluation of n-substituted 1-(5-fluoro-2-pyrimidinyl)piperazine derivatives as potential anti-ischemic agents
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.83 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL57606 | — | — | 1 | 7.92 |
| CHEMBL60814 | — | — | 1 | 7.64 |
| CHEMBL58601 | — | — | 1 | 7.29 |
| CHEMBL59006 | — | — | 1 | 7.28 |
| CHEMBL61177 | — | — | 1 | 7.06 |
| CHEMBL300150 | — | — | 1 | 7.05 |
| CHEMBL60859 | BMY-14802 | — | 1 | 6.95 |
| CHEMBL61304 | — | — | 1 | 6.67 |
| CHEMBL60872 | — | — | 1 | 6.67 |
| CHEMBL301642 | — | — | 1 | 6.64 |
| CHEMBL58282 | — | — | 1 | 6.30 |
| CHEMBL300351 | — | — | 1 | 5.82 |
| CHEMBL57297 | — | — | 1 | 5.46 |
| CHEMBL61303 | — | — | 1 | - |
| CHEMBL299046 | — | — | 1 | - |
| CHEMBL293292 | — | — | 1 | - |
| CHEMBL58283 | — | — | 1 | - |
| CHEMBL293364 | — | — | 1 | - |
| CHEMBL58566 | — | — | 1 | - |
| CHEMBL300556 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL57606 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL60814 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL58601 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL59006 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL61177 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL300150 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL60859 | BMY-14802 | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL61304 | — | IC50 | = | 213.0 | nM | 6.67 |
| CHEMBL60872 | — | IC50 | = | 215.0 | nM | 6.67 |
| CHEMBL301642 | — | IC50 | = | 227.0 | nM | 6.64 |
| CHEMBL58282 | — | IC50 | = | 504.0 | nM | 6.30 |
| CHEMBL300351 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL57297 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL61303 | — | IC50 | > | 45.0 | nM | - |
| CHEMBL299046 | — | IC50 | - | nM | - | |
| CHEMBL293292 | — | IC50 | - | nM | - | |
| CHEMBL58283 | — | IC50 | > | 2.0 | nM | - |
| CHEMBL293364 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL58566 | — | IC50 | > | 1.0 | nM | - |
| CHEMBL300556 | — | IC50 | > | 49.0 | nM | - |