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Assay Detail

CHEMBL808187

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

Binding
Inhibition of [3H]NANM binding to sigma receptor obtained from tissue homogenate preparation of fresh whole rat brain minus cerebellum
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Rigid phencyclidine analogues. Binding to the phencyclidine and sigma 1 receptors.
Moriarty RM, Enache LA, Zhao L, Gilardi R, Mattson MV, Prakash O.
J Med Chem (1998) 41 : 468 -477
PubMed 9484497 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.67 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7393 1 7.89
CHEMBL305881 1 7.36
CHEMBL145722 1 6.50
CHEMBL142600 1 6.48
CHEMBL356757 1 6.44
CHEMBL275528 PHENCYCLIDINE 2.0 1 6.28
CHEMBL284237 DIZOCILPINE 2.0 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7393 IC50 = 13.0 nM 7.89
CHEMBL305881 IC50 = 44.0 nM 7.36
CHEMBL145722 IC50 = 319.0 nM 6.50
CHEMBL142600 IC50 = 330.0 nM 6.48
CHEMBL356757 IC50 = 365.0 nM 6.44
CHEMBL275528 PHENCYCLIDINE IC50 = 530.0 nM 6.28
CHEMBL284237 DIZOCILPINE IC50 = 1700.0 nM 5.77