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Assay Detail

CHEMBL4723549

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

Binding
Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in Sprague-Dawley rat brain membranes by scintillation counting method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL3602)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Small Molecules Selectively Targeting Sigma-1 Receptor for the Treatment of Neurological Diseases.
Ye N,Qin W,Tian S,Xu Q,Wold EA,Zhou J,Zhen XC
J Med Chem (2020) 63 : 15187 -15217
PubMed 33111525 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.86 7.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL814 FLUVOXAMINE 4.0 1 7.44
CHEMBL809 SERTRALINE 4.0 1 7.24
CHEMBL41 FLUOXETINE 4.0 1 6.62
CHEMBL549 CITALOPRAM 4.0 1 6.54
CHEMBL11 IMIPRAMINE 4.0 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL814 FLUVOXAMINE Ki = 36.0 nM 7.44
CHEMBL809 SERTRALINE Ki = 57.0 nM 7.24
CHEMBL41 FLUOXETINE Ki = 240.0 nM 6.62
CHEMBL549 CITALOPRAM Ki = 292.0 nM 6.54
CHEMBL11 IMIPRAMINE Ki = 343.0 nM 6.46