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Assay Detail

CHEMBL4185157

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Binding
Inhibition of full length human APE1 expressed in Escherichia coli BL21/DE3 assessed as inhibition of incision of depurinated supercoiled pUC18 plasmid DNA after 15 mins
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 6.20 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22077 HYCANTHONE 2.0 1 7.10
CHEMBL279014 LUCANTHONE 2.0 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22077 HYCANTHONE IC50 = 80.0 nM 7.10
CHEMBL279014 LUCANTHONE IC50 = 5000.0 nM 5.30