Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL803930

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
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
Yevich JP, Dextraze P, Taylor DP, Moon SL
Bioorg Med Chem Lett (1994) 4 : 1941 -1946
· DOI

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 -