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Assay Detail

CHEMBL4229764

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

Binding
Displacement of [3H]-(+)pentazocine from sigma-1 receptor in guinea pig brain 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 Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL4153)
Type SINGLE PROTEIN
Organism Cavia porcellus

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 8.69 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4250984 1 9.52
CHEMBL4243296 1 8.96
CHEMBL4240868 1 8.74
CHEMBL303336 1 8.70
CHEMBL4243361 1 8.57
CHEMBL4247145 1 8.54
CHEMBL302197 1 8.42
CHEMBL62408 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4250984 Ki = 0.3 nM 9.52
CHEMBL4243296 Ki = 1.1 nM 8.96
CHEMBL4240868 Ki = 1.8 nM 8.74
CHEMBL303336 Ki = 2.0 nM 8.70
CHEMBL4243361 Ki = 2.7 nM 8.57
CHEMBL4247145 Ki = 2.9 nM 8.54
CHEMBL302197 Ki = 3.8 nM 8.42
CHEMBL62408 Ki = 8.0 nM 8.10