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Assay Detail

CHEMBL4839716

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Binding
Binding affinity to Sigma 2-receptor (unknown origin)
8
Total Activities
8
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 intracellular receptor 2 (CHEMBL4105907)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Investigational Drug CT1812, an Antagonist of the Sigma-2 Receptor Complex for Alzheimer's Disease.
Rishton GM, Look GC, Ni ZJ, Zhang J, Wang Y, Huang Y, Wu X, Izzo NJ, LaBarbera KM, Limegrover CS, Rehak C, Yurko R, Catalano SM.
ACS Med Chem Lett (2021) 12 : 1389 -1395
PubMed 34531947 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.76 9.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4853196 1 9.36
CHEMBL4846092 1 8.07
CHEMBL4865307 1 8.05
CHEMBL4867297 1 7.96
CHEMBL4848550 1 7.32
CHEMBL4863873 1 7.30
CHEMBL4876663 1 7.10
CHEMBL4869437 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4853196 Ki = 0.44 nM 9.36
CHEMBL4846092 Ki = 8.5 nM 8.07
CHEMBL4865307 Ki = 9.0 nM 8.05
CHEMBL4867297 Ki = 11.0 nM 7.96
CHEMBL4848550 Ki = 48.0 nM 7.32
CHEMBL4863873 Ki = 50.0 nM 7.30
CHEMBL4876663 Ki = 79.0 nM 7.10
CHEMBL4869437 Ki = 120.0 nM 6.92