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Assay Detail

CHEMBL4185158

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Binding
Inhibition of redox activity of full length N-terminal hexa-His SUMO-fused human APE1 using HEX-labeled THF oligonucleotide as substrate preincubated for 30 to 120 mins followed by substrate addition measured after 15 mins by fluorescence assay
2
Total Activities
2
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 2 5.04 5.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4206043 1 5.07
CHEMBL578390 APX-3330 2.0 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4206043 IC50 = 8500.0 nM 5.07
CHEMBL578390 APX-3330 IC50 = 10000.0 nM 5.00