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Assay Detail

CHEMBL3767807

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

Binding
Displacement of [3H]-pentazocine from sigma 1 receptor in guinea pig brain membrane after 120 mins
8
Total Activities
8
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

Development of sigma-1 (σ1) receptor fluorescent ligands as versatile tools to study σ1 receptors.
Abate C, Riganti C, Pati ML, Ghigo D, Berardi F, Mavlyutov T, Guo LW, Ruoho A.
Eur J Med Chem (2016) 108 : 577 -585
PubMed 26717207 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.51 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL176941 1 10.52
CHEMBL573234 1 9.96
CHEMBL177952 1 9.00
CHEMBL3765740 1 8.44
CHEMBL60542 (+)-PENTAZOCINE 1 8.35
CHEMBL3763396 1 8.28
CHEMBL3763740 1 7.88
CHEMBL2437387 1 5.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL176941 Ki = 0.03 nM 10.52
CHEMBL573234 Ki = 0.11 nM 9.96
CHEMBL177952 Ki = 1.01 nM 9.00
CHEMBL3765740 Ki = 3.61 nM 8.44
CHEMBL60542 (+)-PENTAZOCINE Ki = 4.52 nM 8.35
CHEMBL3763396 Ki = 5.2 nM 8.28
CHEMBL3763740 Ki = 13.1 nM 7.88
CHEMBL2437387 Ki = 2435.0 nM 5.61