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Assay Detail

CHEMBL5138554

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

Binding
Inhibition of human recombinant full-length DNMT1 expressed in Sf9 cells assessed as inhibition of methylated dI-dC formation using 100 ug/ml poly dI-dC and [Me-3H]SAM as substrate incubated for 2 hrs by liquid scintillation counting analysis
1
Total Activities
1
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 1 (CHEMBL1993)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Characterization of Transition-State Analogue Inhibitors against Human DNA Methyltransferase 1.
Lamiable-Oulaidi F, Harijan RK, Shaffer KJ, Crump DR, Sun Y, Du Q, Gulab SA, Khan AA, Luxenburger A, Woolhouse AD, Sidoli S, Tyler PC, Schramm VL.
J Med Chem (2022) 65 : 5462 -5494
PubMed 35324190 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.30 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4170114 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4170114 IC50 = 5000.0 nM 5.30