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Assay Detail

CHEMBL3398686

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

Binding
Inhibition of human purified MPG pre-incubated with compound for 10 mins followed by addition of 1,N6 ethenoadenine containing 32P-labeled duplex oligonucleotide substrates by gel-based excision activity 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-3-methyladenine glycosylase (CHEMBL3396943)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Naturally occurring polyphenol, morin hydrate, inhibits enzymatic activity of N-methylpurine DNA glycosylase, a DNA repair enzyme with various roles in human disease.
Dixon M, Woodrick J, Gupta S, Karmahapatra SK, Devito S, Vasudevan S, Dakshanamurthy S, Adhikari S, Yenugonda VM, Roy R.
Bioorg Med Chem (2015) 23 : 1102 -1111
PubMed 25650313 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.85 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275938 AURINTRICARBOXYLIC ACID 1 6.70
CHEMBL1417019 MITOXANTRONE HYDROCHLORIDE 4.0 1 5.60
CHEMBL1512355 1 5.58
CHEMBL51483 GOSSYPOL 3.0 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275938 AURINTRICARBOXYLIC ACID IC50 = 200.0 nM 6.70
CHEMBL1417019 MITOXANTRONE HYDROCHLORIDE IC50 = 2500.0 nM 5.60
CHEMBL1512355 IC50 = 2600.0 nM 5.58
CHEMBL51483 GOSSYPOL IC50 = 3000.0 nM 5.52