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Assay Detail

CHEMBL846627

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

Binding
Inhibition of specific binding of [3H]NANM of sigma receptor in Guinea pig brain membranes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Tissue Brain
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Sigma non-opioid intracellular receptor 1 (CHEMBL287)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Radiosynthesis, cerebral distribution, and binding of [125I]-1-(p-iodophenyl)-3-(1-adamantyl)guanidine, a ligand for sigma binding sites.
Kimes AS, Wilson AA, Scheffel U, Campbell BG, London ED.
J Med Chem (1992) 35 : 4683 -4689
PubMed 1469697 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.54 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL415284 NALORPHINE 2.0 1 7.32
CHEMBL275707 RIMCAZOLE 2.0 1 6.35
CHEMBL279676 TENOCYCLIDINE 2.0 1 5.96
CHEMBL284237 DIZOCILPINE 2.0 1 -
CHEMBL26 SULPIRIDE 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL415284 NALORPHINE IC50 = 48.0 nM 7.32
CHEMBL275707 RIMCAZOLE IC50 = 450.0 nM 6.35
CHEMBL279676 TENOCYCLIDINE IC50 = 1100.0 nM 5.96
CHEMBL284237 DIZOCILPINE IC50 > 10000.0 nM -
CHEMBL26 SULPIRIDE IC50 > 10000.0 nM -