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Assay Detail

CHEMBL2066852

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

Binding
Inhibition of DNMT1 in human HeLa cell nuclear extract assessed as methylated substrate level by ELISA
2
Total Activities
1
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

New cytosine derivatives as inhibitors of DNA methylation.
Plitta B, Adamska E, Giel-Pietraszuk M, Fedoruk-Wyszomirska A, Naskręt-Barciszewska M, Markiewicz WT, Barciszewski J.
Eur J Med Chem (2012) 55 : 243 -254
PubMed 22854677 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.66 4.66
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2063048 2 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2063048 IC50 = 22000.0 nM 4.66
CHEMBL2063048 Inhibition - % -