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Assay Detail

CHEMBL1036447

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

Binding
Inhibition of human recombinant DNMT3b2 at 45 uM
7
Total Activities
6
Compounds Tested
2
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 3B (CHEMBL6095)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Constrained (l-)-S-adenosyl-l-homocysteine (SAH) analogues as DNA methyltransferase inhibitors.
Isakovic L, Saavedra OM, Llewellyn DB, Claridge S, Zhan L, Bernstein N, Vaisburg A, Elowe N, Petschner AJ, Rahil J, Beaulieu N, Gauthier F, MacLeod AR, Delorme D, Besterman JM, Wahhab A.
Bioorg Med Chem Lett (2009) 19 : 2742 -2746
PubMed 19364644 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 6 - -
IC50 1 6.22 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL555352 1 6.22
CHEMBL563803 1 -
CHEMBL551578 1 -
CHEMBL551499 1 -
CHEMBL559710 2 -
CHEMBL564490 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL555352 IC50 = 600.0 nM 6.22
CHEMBL563803 Inhibition = 42.0 % -
CHEMBL551578 Inhibition = 50.0 % -
CHEMBL551499 Inhibition = 51.0 % -
CHEMBL559710 Inhibition = - % -
CHEMBL559710 Inhibition = 16.0 % -
CHEMBL564490 Inhibition = 32.0 % -