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Assay Detail

CHEMBL945288

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

Binding
Displacement of [3H](+)-pentazocine from sigma1 receptor in guinea pig brain membrane by liquid scintillation counting
15
Total Activities
13
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

Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter.
Tu Z, Efange SM, Xu J, Li S, Jones LA, Parsons SM, Mach RH.
J Med Chem (2009) 52 : 1358 -1369
PubMed 19203271 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.03 7.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129530 1 7.67
CHEMBL516814 1 7.67
CHEMBL20730 VESAMICOL 1 7.59
CHEMBL461956 1 7.51
CHEMBL473129 3 6.73
CHEMBL473546 1 6.66
CHEMBL473547 1 6.53
CHEMBL473751 1 -
CHEMBL473548 1 -
CHEMBL87379 BENZOVESAMICOL 1 -
CHEMBL461783 1 -
CHEMBL510679 1 -
CHEMBL462659 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129530 Ki = 21.6 nM 7.67
CHEMBL516814 Ki = 21.3 nM 7.67
CHEMBL20730 VESAMICOL Ki = 25.8 nM 7.59
CHEMBL461956 Ki = 30.6 nM 7.51
CHEMBL473129 Ki = 185.97 nM 6.73
CHEMBL473129 Ki = 191.1 nM 6.72
CHEMBL473546 Ki = 219.6 nM 6.66
CHEMBL473547 Ki = 297.7 nM 6.53
CHEMBL473129 Ki = 658.6 nM 6.18
CHEMBL473751 Ki - -
CHEMBL473548 Ki - -
CHEMBL87379 BENZOVESAMICOL Ki - -
CHEMBL461783 Ki - -
CHEMBL510679 Ki - -
CHEMBL462659 Ki - -