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Assay Detail

CHEMBL803924

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

Binding
Binding affinity towards sigma receptor in guinea pig brain membrane was determined by using [3H]DTG as the radioligand
7
Total Activities
7
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 Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL287)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Trishomocubanes, a new class of selective and high affinity ligands for the sigma binding site
Kassiou M, Nguyen VH, Knott R, Christie MJ, Hambley TW
Bioorg Med Chem Lett (1996) 6 : 595 -600
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.45 8.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL541347 1 8.16
CHEMBL660 AMANTADINE 4.0 1 7.69
CHEMBL538300 1 7.52
CHEMBL552794 1 7.46
CHEMBL539310 1 7.24
CHEMBL538057 1 7.10
CHEMBL348313 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL541347 Ki = 6.9 nM 8.16
CHEMBL660 AMANTADINE Ki = 20.25 nM 7.69
CHEMBL538300 Ki = 30.1 nM 7.52
CHEMBL552794 Ki = 34.5 nM 7.46
CHEMBL539310 Ki = 58.2 nM 7.24
CHEMBL538057 Ki = 78.7 nM 7.10
CHEMBL348313 Ki = 109.0 nM 6.96