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Assay Detail

CHEMBL4334315

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

Binding
Inhibition of recombinant human N-terminal FLAG-tagged TET1 (1418 to 2136 residues) expressed in baculovirus infected sf9 cells assessed as reduction in oxidation of methylated dsDNA after 2 hrs by chemiluminescence assay
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

Methylcytosine dioxygenase TET1 (CHEMBL4523402)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cytosine-Based TET Enzyme Inhibitors.
Chua GNL, Wassarman KL, Sun H, Alp JA, Jarczyk EI, Kuzio NJ, Bennett MJ, Malachowsky BG, Kruse M, Kennedy AJ.
ACS Med Chem Lett (2019) 10 : 180 -185
PubMed 30783500 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.48 4.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4457636 1 4.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4457636 IC50 = 33000.0 nM 4.48