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Assay Detail

CHEMBL4185149

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Binding
Inhibition of human APE1 using a 5'-TAMRA labelled THF abasic site double-stranded oligodeoxynucleotide as substrate in presence of Mg2+ by fluorescence polarization displacement assay
5
Total Activities
5
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 repair nuclease/redox regulator APEX1 (CHEMBL5619)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Inhibitors of nuclease and redox activity of apurinic/apyrimidinic endonuclease 1/redox effector factor 1 (APE1/Ref-1).
Laev SS, Salakhutdinov NF, Lavrik OI.
Bioorg Med Chem (2017) 25 : 2531 -2544
PubMed 28161249 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.73 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1346456 1 6.40
CHEMBL1601846 1 6.40
CHEMBL1597042 1 5.55
CHEMBL1497243 1 5.17
CHEMBL1541779 1 5.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1346456 IC50 = 400.0 nM 6.40
CHEMBL1601846 IC50 = 400.0 nM 6.40
CHEMBL1597042 IC50 = 2800.0 nM 5.55
CHEMBL1497243 IC50 = 6800.0 nM 5.17
CHEMBL1541779 IC50 = 7070.0 nM 5.15