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Assay Detail

CHEMBL4625173

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

Binding
Inhibition of murine DNMT3A catalytic domain-mediated DNA methylation using 5'-6FAM-tagged 30-mer duplex DNA (17 AT bp) as substrate preincubated for 30 mins followed by enzyme addition
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

DNA (cytosine-5)-methyltransferase 3A (CHEMBL3108652)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Novel anticancer drug curaxin CBL0137 impairs DNA methylation by eukaryotic DNA methyltransferase Dnmt3a.
Sergeev A, Vorobyov A, Yakubovskaya M, Kirsanova O, Gromova E.
Bioorg Med Chem Lett (2020) 30 : 127296 -127296
PubMed 32631516 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.29 5.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL53463 DOXORUBICIN 4.0 1 5.52
CHEMBL4640631 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL53463 DOXORUBICIN IC50 = 3000.0 nM 5.52
CHEMBL4640631 IC50 = 9000.0 nM 5.05