Assay Detail
Functional
CHEMBL780358
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of (+)-[3H]-3-PPP from rat cortical sigma site
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Sigma non-opioid intracellular receptor 1 (CHEMBL3602) ↗| Type | SINGLE PROTEIN |
| Organism | Rattus norvegicus |
Publication
Synthesis and biological characterization of alpha-(4-fluorophenyl)-4-(5-fluoro-2-pyrimidinyl)-1-piperazinebutanol and analogues as potential atypical antipsychotic agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 6.99 | 7.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL139595 | — | — | 1 | 7.66 |
| CHEMBL141854 | — | — | 1 | 7.62 |
| CHEMBL140650 | — | — | 1 | 7.58 |
| CHEMBL141670 | — | — | 1 | 7.58 |
| CHEMBL137870 | — | — | 1 | 7.24 |
| CHEMBL141226 | — | — | 1 | 7.09 |
| CHEMBL141922 | — | — | 1 | 7.07 |
| CHEMBL141912 | — | — | 1 | 6.96 |
| CHEMBL60859 | BMY-14802 | — | 1 | 6.95 |
| CHEMBL141455 | — | — | 1 | 6.92 |
| CHEMBL335348 | — | — | 1 | 6.89 |
| CHEMBL140656 | — | — | 1 | 6.89 |
| CHEMBL140712 | — | — | 1 | 6.80 |
| CHEMBL443482 | — | — | 1 | 6.72 |
| CHEMBL141523 | — | — | 1 | 6.43 |
| CHEMBL140872 | — | — | 1 | 6.37 |
| CHEMBL479 | THIORIDAZINE | 4.0 | 1 | 6.12 |
| CHEMBL342484 | — | — | 1 | - |
| CHEMBL138186 | — | — | 1 | - |
| CHEMBL140833 | — | — | 1 | - |
| CHEMBL344577 | — | — | 1 | - |
| CHEMBL140831 | — | — | 1 | - |
| CHEMBL137967 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL139595 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL141854 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL140650 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL141670 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL137870 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL141226 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL141922 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL141912 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL60859 | BMY-14802 | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL141455 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL335348 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL140656 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL140712 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL443482 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL141523 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL140872 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL479 | THIORIDAZINE | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL342484 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL138186 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL140833 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL344577 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL140831 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL137967 | — | IC50 | ~ | 1000.0 | nM | - |