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Assay Detail

CHEMBL809049

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

Binding
In vitro binding affinity at Sigma opioid receptor type 2 on guinea pig brain membranes by [3H]DTG displacement in the presence of [3H]pentazocine.
4
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
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 SAR of 1-alkyl-2-phenylethylamine derivatives designed from N,N-dipropyl-4-methoxy-3-(2-phenylethoxy)phenylethylamine to discover sigma(1) ligands.
Nakazato A, Kumagai T, Ohta K, Chaki S, Okuyama S, Tomisawa K.
J Med Chem (1999) 42 : 3965 -3970
PubMed 10508444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 6.79 7.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL521582 1 7.07
CHEMBL540331 2 6.72
CHEMBL541091 1 6.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL521582 IC50 = 85.0 nM 7.07
CHEMBL540331 IC50 = 190.0 nM 6.72
CHEMBL540331 IC50 = 200.0 nM 6.70
CHEMBL541091 IC50 = 210.0 nM 6.68