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Assay Detail

CHEMBL3767808

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

Binding
Displacement of [3H]-DTG from sigma 2 receptor in Wistar hannover rat liver membrane after 120 mins
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Membrane
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 7.46 8.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2437387 1 8.37
CHEMBL176941 1 7.75
CHEMBL282433 DITOLYLGUANIDINE 1 7.45
CHEMBL3763740 1 7.42
CHEMBL3763396 1 7.34
CHEMBL3765740 1 7.32
CHEMBL177952 1 7.31
CHEMBL573234 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2437387 Ki = 4.24 nM 8.37
CHEMBL176941 Ki = 17.9 nM 7.75
CHEMBL282433 DITOLYLGUANIDINE Ki = 35.4 nM 7.45
CHEMBL3763740 Ki = 38.4 nM 7.42
CHEMBL3763396 Ki = 45.6 nM 7.34
CHEMBL3765740 Ki = 48.3 nM 7.32
CHEMBL177952 Ki = 48.7 nM 7.31
CHEMBL573234 Ki = 179.0 nM 6.75