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Assay Detail

CHEMBL5116794

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

Binding
Binding affinity to sigma 2 receptor (unknown origin) assessed as inhibition constant by radioligand binding assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sigma intracellular receptor 2 (CHEMBL4105907)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and biological evaluation of novel aminopropylcarboxamide derivatives as sigma ligands.
Zampieri D, Fortuna S, Romano M, Amata E, Dichiara M, Marrazzo A, Pasquinucci L, Turnaturi R, Mamolo MG.
Bioorg Med Chem Lett (2022) 72 : 128860 -128860
PubMed 35724925 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.20 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5169420 1 8.00
CHEMBL5187029 1 7.80
CHEMBL54 HALOPERIDOL 4.0 1 7.80
CHEMBL282433 DITOLYLGUANIDINE 1 7.75
CHEMBL5201355 1 7.68
CHEMBL5182253 1 7.34
CHEMBL5186843 1 6.97
CHEMBL5207122 1 6.90
CHEMBL5206034 1 5.97
CHEMBL100116 PENTAZOCINE 4.0 1 5.83
CHEMBL5201238 1 -
CHEMBL38874 DAMGO 1 -
CHEMBL567175 NALTRINDOLE 1 -
CHEMBL290543 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5169420 Ki = 9.9 nM 8.00
CHEMBL5187029 Ki = 16.0 nM 7.80
CHEMBL54 HALOPERIDOL Ki = 16.0 nM 7.80
CHEMBL282433 DITOLYLGUANIDINE Ki = 18.0 nM 7.75
CHEMBL5201355 Ki = 21.0 nM 7.68
CHEMBL5182253 Ki = 46.0 nM 7.34
CHEMBL5186843 Ki = 106.0 nM 6.97
CHEMBL5207122 Ki = 126.0 nM 6.90
CHEMBL5206034 Ki = 1067.0 nM 5.97
CHEMBL100116 PENTAZOCINE Ki = 1465.0 nM 5.83
CHEMBL5201238 Ki > 5000.0 nM -
CHEMBL38874 DAMGO Ki - -
CHEMBL567175 NALTRINDOLE Ki - -
CHEMBL290543 Ki - -