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Assay Detail

CHEMBL4723541

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

Binding
Displacement of [3H]-(+)-pentazocine from sigma 1 receptor in rat liver membranes incubated for 60 mins in presence of [3H]DTG by radioactivity method
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
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 8.87 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39900 SPIPETHIANE 1 9.30
CHEMBL4796879 1 8.85
CHEMBL4763051 1 8.85
CHEMBL4744344 1 8.84
CHEMBL4760729 1 8.53

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39900 SPIPETHIANE Ki = 0.5 nM 9.30
CHEMBL4796879 Ki = 1.41 nM 8.85
CHEMBL4763051 Ki = 1.4 nM 8.85
CHEMBL4744344 Ki = 1.45 nM 8.84
CHEMBL4760729 Ki = 2.95 nM 8.53