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Assay Detail

CHEMBL3418014

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

Binding
Inhibition of His6-tagged human recombinant DNMT3b expressed in insect Sf9 cells assessed as reduction in DNA methyltransferase activity using 5'-biotinylated 45-bp unmethylated or hemimethylated oligonucleotide substrates and [3H]-AdoMet by liquid scintillation counting method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

DNA (cytosine-5)-methyltransferase 3B (CHEMBL6095)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting DNA methylation with small molecules: what's next?
Erdmann A, Halby L, Fahy J, Arimondo PB.
J Med Chem (2015) 58 : 2569 -2583
PubMed 25406944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.71 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2106789 NANAFROCIN 2.0 1 6.30
CHEMBL2336409 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2106789 NANAFROCIN IC50 = 500.0 nM 6.30
CHEMBL2336409 IC50 = 7500.0 nM 5.12