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Assay Detail

CHEMBL809862

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

Binding
Binding affinity against Sigma opioid receptor type 2 in rat liver membranes using [3H]DTG (DuPont-NEN) as radioligand in the presence of (+)-pentazocine (100 nM)
9
Total Activities
6
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 Expert

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL3602)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Hydroxylated decahydroquinolines as ligands for the vesicular acetylcholine transporter: synthesis and biological evaluation.
Efange SM, Khare AB, Mach RH, Parsons SM.
J Med Chem (1999) 42 : 2862 -2869
PubMed 10425095 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.93 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL316520 3 7.60
CHEMBL20730 VESAMICOL 1 7.47
CHEMBL97524 2 7.39
CHEMBL95857 1 6.90
CHEMBL50880 1 6.72
CHEMBL95701 1 6.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL316520 Ki = 25.0 nM 7.60
CHEMBL20730 VESAMICOL Ki = 34.0 nM 7.47
CHEMBL97524 Ki = 41.0 nM 7.39
CHEMBL95857 Ki = 127.0 nM 6.90
CHEMBL50880 Ki = 190.0 nM 6.72
CHEMBL97524 Ki = 233.0 nM 6.63
CHEMBL95701 Ki = 363.0 nM 6.44
CHEMBL316520 Ki = 553.0 nM 6.26
CHEMBL316520 Ki > 1000.0 nM -