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Assay Detail

CHEMBL4185147

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Binding
Inhibition of N-terminal hexa-His tagged human APE1 expressed in Escherichia coli BL21 (Rosetta) using fluorescein-dabcyl-containing oligonucleotide as substrate measured over 5 mins by high-throughput fluorescence assay
3
Total Activities
3
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 3 5.75 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2349528 1 5.80
CHEMBL1443537 1 5.77
CHEMBL1453126 1 5.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2349528 IC50 = 1600.0 nM 5.80
CHEMBL1443537 IC50 = 1700.0 nM 5.77
CHEMBL1453126 IC50 = 2100.0 nM 5.68