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Assay Detail

CHEMBL5164049

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

Binding
Binding affinity to sigma 1 receptor expressed in guinea pig brain membrane assessed as inhibition constant
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL4153)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Preparation of novel analogs of 2-arylpiperidines and evaluation of their sigma receptor binding affinities.
Walby GD, Martin SF.
Eur J Med Chem (2022) 235 : 114310 -114310
PubMed 35395511 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.31 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5175530 1 6.64
CHEMBL5190189 1 6.61
CHEMBL1698776 1 6.08
CHEMBL5189158 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5175530 Ki = 230.0 nM 6.64
CHEMBL5190189 Ki = 248.0 nM 6.61
CHEMBL1698776 Ki = 841.0 nM 6.08
CHEMBL5189158 Ki = 1279.0 nM 5.89