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Assay Detail

CHEMBL888902

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 membrane after 90 mins
6
Total Activities
6
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 Intermediate

Target

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

Publication

Fluorine-18-labeled benzamide analogues for imaging the sigma2 receptor status of solid tumors with positron emission tomography.
Tu Z, Xu J, Jones LA, Li S, Dumstorff C, Vangveravong S, Chen DL, Wheeler KT, Welch MJ, Mach RH.
J Med Chem (2007) 50 : 3194 -3204
PubMed 17579383 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.58 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL226539 1 6.48
CHEMBL226540 1 5.97
CHEMBL387741 1 5.89
CHEMBL227071 1 5.67
CHEMBL226538 1 4.82
CHEMBL389261 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL226539 Ki = 330.0 nM 6.48
CHEMBL226540 Ki = 1076.0 nM 5.97
CHEMBL387741 Ki = 1300.0 nM 5.89
CHEMBL227071 Ki = 2150.0 nM 5.67
CHEMBL226538 Ki = 15300.0 nM 4.82
CHEMBL389261 Ki = 22750.0 nM 4.64