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Assay Detail

CHEMBL5130682

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

Binding
Displacement of thiazole orange from c-kit1 G4 quadruplex d(DNA AGG GAG GGC GCT GGG AGG AGG G) DNA (unknown origin) assessed as relative affinity by fluorescent intercalator displacement assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Not specified
Confidence 3 — Cell-line / Tissue
Curated By Autocuration

Target

quadruplex DNA (CHEMBL3832742)
Type NUCLEIC-ACID
Organism Homo sapiens

Publication

Balancing Affinity, Selectivity, and Cytotoxicity of Hydrazone-Based G-Quadruplex Ligands for Activation of Interferon β Genes in Cancer Cells.
Marzano S, Miglietta G, Morigi R, Marinello J, Arleo A, Procacci M, Locatelli A, Leoni A, Pagano B, Randazzo A, Amato J, Capranico G.
J Med Chem (2022) 65 : 12055 -12067
PubMed 36074772 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.81 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5191417 1 5.92
CHEMBL5180396 1 5.89
CHEMBL5177572 1 5.85
CHEMBL5182391 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5191417 IC50 = 1200.0 nM 5.92
CHEMBL5180396 IC50 = 1300.0 nM 5.89
CHEMBL5177572 IC50 = 1400.0 nM 5.85
CHEMBL5182391 IC50 = 2700.0 nM 5.57