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Assay Detail

CHEMBL4723535

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

Binding
Displacement of [3H]DTG from sigma 2 receptor in Sprague-Dawley rat brain membranes in presence of (+)-pentazocine 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 intracellular receptor 2 (CHEMBL4105864)
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 5.22 5.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL11 IMIPRAMINE 4.0 1 5.68
CHEMBL809 SERTRALINE 4.0 1 5.28
CHEMBL549 CITALOPRAM 4.0 1 5.27
CHEMBL814 FLUVOXAMINE 4.0 1 5.07
CHEMBL41 FLUOXETINE 4.0 1 4.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL11 IMIPRAMINE Ki = 2107.0 nM 5.68
CHEMBL809 SERTRALINE Ki = 5297.0 nM 5.28
CHEMBL549 CITALOPRAM Ki = 5410.0 nM 5.27
CHEMBL814 FLUVOXAMINE Ki = 8439.0 nM 5.07
CHEMBL41 FLUOXETINE Ki = 16100.0 nM 4.79