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Assay Detail

CHEMBL2438375

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 membranes
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Development of 3,4-dihydroisoquinolin-1(2H)-one derivatives for the Positron Emission Tomography (PET) imaging of σ₂ receptors.
Abate C, Selivanova SV, Müller A, Krämer SD, Schibli R, Marottoli R, Perrone R, Berardi F, Niso M, Ametamey SM.
Eur J Med Chem (2013) 69 : 920 -930
PubMed 24161678 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 8.02 8.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2437383 1 8.45
CHEMBL2437387 1 8.37
CHEMBL2437384 1 8.24
CHEMBL2437386 1 8.03
CHEMBL2437385 1 7.79
CHEMBL2437382 1 7.70
CHEMBL282433 DITOLYLGUANIDINE 1 7.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2437383 Ki = 3.56 nM 8.45
CHEMBL2437387 Ki = 4.24 nM 8.37
CHEMBL2437384 Ki = 5.74 nM 8.24
CHEMBL2437386 Ki = 9.24 nM 8.03
CHEMBL2437385 Ki = 16.3 nM 7.79
CHEMBL2437382 Ki = 20.1 nM 7.70
CHEMBL282433 DITOLYLGUANIDINE Ki = 25.7 nM 7.59