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Assay Detail

CHEMBL809042

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

Binding
Binding effinity for sigma receptor using 2 nM of [3H]DTG as radioligand, in membranes from brain minus cerebellum
5
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Substituted 3-phenylpiperidines: new centrally acting dopamine autoreceptor antagonists.
Sonesson C, Waters N, Svensson K, Carlsson A, Smith MW, Piercey MF, Meier E, Wikström H.
J Med Chem (1993) 36 : 3188 -3196
PubMed 8230107 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 6.76 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110821 1 8.22
CHEMBL90359 1 7.50
CHEMBL276500 2 6.37
CHEMBL107492 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110821 IC50 = 6.0 nM 8.22
CHEMBL90359 IC50 = 32.0 nM 7.50
CHEMBL276500 IC50 = 430.0 nM 6.37
CHEMBL276500 IC50 = 940.0 nM 6.03
CHEMBL107492 IC50 = 2200.0 nM 5.66