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Assay Detail

CHEMBL5252007

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

Binding
Binding affinity to sigma 2 receptor in human MCF7 cells assessed as displacement of compound by measuring inhibition constant of DTG incubated for 120 mins by saturation binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MCF7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma intracellular receptor 2 (CHEMBL4105907)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of Fluorescent 4-[4-(3<i>H</i>-Spiro[isobenzofuran-1,4'-piperidin]-1'-yl)butyl]indolyl Derivatives as High-Affinity Probes to Enable the Study of σ Receptors via Fluorescence-Based Techniques.
Abatematteo FS, Majellaro M, Montsch B, Prieto-Díaz R, Niso M, Contino M, Stefanachi A, Riganti C, Mangiatordi GF, Delre P, Heffeter P, Sotelo E, Abate C.
J Med Chem (2023) 66 : 3798 -3817
PubMed 36919956 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.87 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5278003 1 9.24
CHEMBL5290452 1 8.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5278003 Ki = 0.58 nM 9.24
CHEMBL5290452 Ki = 3.14 nM 8.50