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Assay Detail

CHEMBL4676328

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

Binding
Displacement of [3H]-di-o-tolylguanidine from Sigma 2 receptor in rat liver membrane incubated for 120 mins by solid scintillation counting method
14
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Liver
Subcellular Cell membrane
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma intracellular receptor 2 (CHEMBL4105864)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Fluorinated 2-Arylcyclopropan-1-amines - A new class of sigma receptor ligands.
Schinor B,Hruschka S,Daniliuc CG,Schepmann D,Wünsch B,Haufe G
Bioorg Med Chem (2020) 28 : 115726 -115726
PubMed 33007549 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 5.73 7.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4741170 2 7.02
CHEMBL1196613 2 5.92
CHEMBL1190691 1 5.70
CHEMBL4754599 2 5.64
CHEMBL561746 1 5.51
CHEMBL4758101 1 5.51
CHEMBL3989843 TRANYLCYPROMINE 4.0 1 5.21
CHEMBL4741351 2 -
CHEMBL4756207 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4741170 Ki = 95.0 nM 7.02
CHEMBL4741170 Ki = 911.0 nM 6.04
CHEMBL1196613 Ki = 1200.0 nM 5.92
CHEMBL1190691 Ki = 2000.0 nM 5.70
CHEMBL4754599 Ki = 2300.0 nM 5.64
CHEMBL1196613 Ki = 2400.0 nM 5.62
CHEMBL561746 Ki = 3100.0 nM 5.51
CHEMBL4758101 Ki = 3100.0 nM 5.51
CHEMBL3989843 TRANYLCYPROMINE Ki = 6200.0 nM 5.21
CHEMBL4754599 Ki = 7100.0 nM 5.15
CHEMBL4741351 Ki - -
CHEMBL4741351 Ki - -
CHEMBL4756207 Ki - -
CHEMBL4756207 Ki - -