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Assay Detail

CHEMBL4229765

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

Binding
Displacement of [3H]-DTG from sigma-2 receptor in rat liver membranes after 180 mins by scintillation counting method
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 9 — Direct single protein target
Curated By Autocuration

Target

Sigma intracellular receptor 2 (CHEMBL4105864)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Quest for Novel Chemical Entities through Incorporation of Silicon in Drug Scaffolds.
Ramesh R, Reddy DS.
J Med Chem (2018) 61 : 3779 -3798
PubMed 29039662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.23 8.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4240868 1 8.26
CHEMBL4250984 1 7.72
CHEMBL62408 1 7.47
CHEMBL4247145 1 7.41
CHEMBL303336 1 7.36
CHEMBL302197 1 6.69
CHEMBL4243296 1 6.61
CHEMBL4243361 1 6.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4240868 Ki = 5.5 nM 8.26
CHEMBL4250984 Ki = 19.0 nM 7.72
CHEMBL62408 Ki = 34.0 nM 7.47
CHEMBL4247145 Ki = 39.0 nM 7.41
CHEMBL303336 Ki = 44.0 nM 7.36
CHEMBL302197 Ki = 206.0 nM 6.69
CHEMBL4243296 Ki = 243.0 nM 6.61
CHEMBL4243361 Ki = 460.0 nM 6.34