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Assay Detail

CHEMBL1036409

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

Binding
Inhibition of human recombinant DNMT3b2 expressed in baculovirus infected high five insect cells
20
Total Activities
20
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 3B (CHEMBL6095)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

SAR around (l)-S-adenosyl-l-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes.
Saavedra OM, Isakovic L, Llewellyn DB, Zhan L, Bernstein N, Claridge S, Raeppel F, Vaisburg A, Elowe N, Petschner AJ, Rahil J, Beaulieu N, MacLeod AR, Delorme D, Besterman JM, Wahhab A.
Bioorg Med Chem Lett (2009) 19 : 2747 -2751
PubMed 19362833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.52 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL552309 1 6.52
CHEMBL418052 S-ADENOSYLHOMOCYSTEINE 1 6.52
CHEMBL555352 1 6.22
CHEMBL560105 1 6.22
CHEMBL560505 1 6.05
CHEMBL560045 1 6.00
CHEMBL556265 1 6.00
CHEMBL563024 1 5.70
CHEMBL549412 1 5.70
CHEMBL552246 1 5.52
CHEMBL560306 1 5.44
CHEMBL561047 1 5.17
CHEMBL538692 1 5.17
CHEMBL563570 1 4.55
CHEMBL552763 1 4.54
CHEMBL563946 1 4.35
CHEMBL564768 1 4.24
CHEMBL558406 1 -
CHEMBL558882 1 -
CHEMBL559715 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL552309 IC50 = 300.0 nM 6.52
CHEMBL418052 S-ADENOSYLHOMOCYSTEINE IC50 = 300.0 nM 6.52
CHEMBL555352 IC50 = 600.0 nM 6.22
CHEMBL560105 IC50 = 600.0 nM 6.22
CHEMBL560505 IC50 = 900.0 nM 6.05
CHEMBL560045 IC50 = 1000.0 nM 6.00
CHEMBL556265 IC50 = 1000.0 nM 6.00
CHEMBL563024 IC50 = 2000.0 nM 5.70
CHEMBL549412 IC50 = 2000.0 nM 5.70
CHEMBL552246 IC50 = 3000.0 nM 5.52
CHEMBL560306 IC50 = 3600.0 nM 5.44
CHEMBL561047 IC50 = 6800.0 nM 5.17
CHEMBL538692 IC50 = 6800.0 nM 5.17
CHEMBL563570 IC50 = 28000.0 nM 4.55
CHEMBL552763 IC50 = 29000.0 nM 4.54
CHEMBL563946 IC50 = 45000.0 nM 4.35
CHEMBL564768 IC50 = 57200.0 nM 4.24
CHEMBL558406 IC50 = 500000.0 nM -
CHEMBL558882 IC50 = 256000.0 nM -
CHEMBL559715 IC50 > 1000000.0 nM -