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Assay Detail

CHEMBL4606698

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

Binding
Inhibition of human recombinant DNMT1 expressed in baculovirus infected insect cells using CpG site containing internally quenched hairpin oligonucleotide DNA substrate and SAM incubated for 30 mins by kinetic fluorogenic assay
4
Total Activities
4
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

DNA (cytosine-5)-methyltransferase 1 (CHEMBL1993)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Guided Identification of DNMT3B Inhibitors.
Newton AS, Faver JC, Micevic G, Muthusamy V, Kudalkar SN, Bertoletti N, Anderson KS, Bosenberg MW, Jorgensen WL.
ACS Med Chem Lett (2020) 11 : 971 -976
PubMed 32435413 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.56 4.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4640870 1 4.57
CHEMBL4649221 1 4.54
CHEMBL4641323 1 -
CHEMBL4644275 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4640870 IC50 = 27200.0 nM 4.57
CHEMBL4649221 IC50 = 28500.0 nM 4.54
CHEMBL4641323 IC50 - -
CHEMBL4644275 IC50 - -