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Assay Detail

CHEMBL5251992

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

Binding
Binding affinity to sigma 1 receptor (unknown origin) assessed as inhibition constant
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL287)
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 4 9.05 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3763396 1 10.52
CHEMBL53325 1 9.42
CHEMBL5272035 1 8.27
CHEMBL61479 SIRAMESINE 2.0 1 7.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3763396 Ki = 0.03 nM 10.52
CHEMBL53325 Ki = 0.38 nM 9.42
CHEMBL5272035 Ki = 5.37 nM 8.27
CHEMBL61479 SIRAMESINE Ki = 10.5 nM 7.98