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Assay Detail

CHEMBL3607245

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

Binding
Inhibition of human C-terminal DNMT3A after 1 hr by fluorescence 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 3A (CHEMBL1992)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of new non nucleoside inhibitors of DNMT3A.
Erdmann A, Menon Y, Gros C, Molinier N, Novosad N, Samson A, Gregoire JM, Long C, Ausseil F, Halby L, Arimondo PB.
Bioorg Med Chem (2015) 23 : 5946 -5953
PubMed 26220519 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.66 6.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2336409 1 6.05
CHEMBL3605964 1 5.68
CHEMBL3605935 1 5.52
CHEMBL3605951 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2336409 EC50 = 900.0 nM 6.05
CHEMBL3605964 EC50 = 2100.0 nM 5.68
CHEMBL3605935 EC50 = 3000.0 nM 5.52
CHEMBL3605951 EC50 = 4000.0 nM 5.40