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Assay Detail

CHEMBL3389217

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Binding
Inhibition of human APE1 after 25 mins by fluorescence assay
7
Total Activities
7
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

DNA repair and redox activities and inhibitors of apurinic/apyrimidinic endonuclease 1/redox effector factor 1 (APE1/Ref-1): a comparative analysis and their scope and limitations toward anticancer drug development.
Kaur G, Cholia RP, Mantha AK, Kumar R.
J Med Chem (2014) 57 : 10241 -10256
PubMed 25280182 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.90 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL109037 1 6.96
CHEMBL1160025 1 6.60
CHEMBL164 MYRICETIN 1 6.50
CHEMBL1870764 1 5.52
CHEMBL1524472 1 5.40
CHEMBL279014 LUCANTHONE 2.0 1 5.30
CHEMBL275938 AURINTRICARBOXYLIC ACID 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL109037 IC50 = 110.0 nM 6.96
CHEMBL1160025 IC50 = 250.0 nM 6.60
CHEMBL164 MYRICETIN IC50 = 320.0 nM 6.50
CHEMBL1870764 IC50 = 3000.0 nM 5.52
CHEMBL1524472 IC50 = 4000.0 nM 5.40
CHEMBL279014 LUCANTHONE IC50 = 5000.0 nM 5.30
CHEMBL275938 AURINTRICARBOXYLIC ACID IC50 = 10000.0 nM 5.00