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Fluorescence-Based APE1 Endonuclease Activity Assay from Article 10.1111/cbdd.12826: "Structure-based virtual screening toward the discovery of novel inhibitors of the DNA repair activity of the human apurinic/apyrimidinic endonuclease 1."
Assay data:3 Active, 1 Activity ≤ 1 µM, 3 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by Target
Electrophoretic Mobility Shift Assays (EMSAs) from Article 10.1021/bi400179m: "Inhibition of apurinic/apyrimidinic endonuclease I's redox activity revisited."
Assay data:1 Active, 2 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by Target
Gel-Based Assay from Article 10.1021/bi300490r: "Identification and characterization of human apurinic/apyrimidinic endonuclease-1 inhibitors."
Assay data:3 Active, 6 Tested
SummaryCompounds, ActivePubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
Molecular Beacon Assay from Article 10.1021/bi300490r: "Identification and characterization of human apurinic/apyrimidinic endonuclease-1 inhibitors."
Assay data:7 Active, 5 Activity ≤ 1 µM, 12 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMPubMed CitationRelated BioAssays by DepositorRelated BioAssays by Target
High-Throughput Screening and IC50 Determinations from Article 10.1124/mol.107.042622: "Potent inhibition of human apurinic/apyrimidinic endonuclease 1 by arylstibonic acids."
Assay data:4 Active, 4 Activity ≤ 1 µM, 4 Tested
APE1 Inhibition Assay from Article 10.1021/jm800739m: "Pharmacophore guided discovery of small-molecule human apurinic/apyrimidinic endonuclease 1 inhibitors."
Assay data:16 Active, 35 Tested
Inhibition Assay from US Patent US9624235: "Compounds and methods for inhibition of AP endonuclease-1/redox factor-1 (HAPE1) activity"
Assay data:8 Active, 6 Activity ≤ 1 µM, 15 Tested
SummaryCompounds, ActiveCompounds, activity ≤ 1 µMRelated BioAssays by Target
Inhibition of APE1 in human ST8814 cells assessed as effect on MMS-induced DNA damage by measuring tail DNA level at 100 uM after 1 hr in presence of MMS by comet assay (Rvb = 16%)
Assay data:7 Tested
SummaryPubMed CitationRelated BioAssays by Target
Inhibition of full length human APE1 assessed as reduction in endonuclease activity by measuring DNA cleavage of abasic sites using 6-FAM labelled two annealed oligonucleotides as AP site mimic substrate by fluorescence-based assay
Assay data:11 Active, 22 Tested
RNAi screen for vemurafenib enhancer genes in BRAFV600 melanoma - Primary Screen
Assay data:790 Active, 18119 Tested
Summary
Inhibition of APE1 (unknown origin) assessed as reduction in AP endonuclease activity at 100 uM
Assay data:1 Tested
Binding affinity to APE1 (unknown origin) by SPR assay
Assay data:1 Active, 1 Activity ≤ 1 µM, 1 Tested
Inhibition of His-tagged human APE1 expressed in Escherichia coli M15 assessed as reduction in cleavage of 26 mer substrate to 13 mer products pre-incubated for 30 mins before substrate addition for 15 mins using 5' end [32P] AP site containing 26 mer oligonucleotide by polyacrylamide gel electrophoresis
Assay data:4 Tested
Binding affinity to full length human APE1 expressed in Escherichia coli BL21/DE3
Assay data:3 Active, 1 Activity ≤ 1 nM, 3 Activity ≤ 1 µM, 3 Tested
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
Assay data:2 Active, 2 Tested
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
Assay data:2 Active, 1 Activity ≤ 1 µM, 2 Tested
Inhibition of APE1 in human HeLa cells
Assay data:1 Active, 1 Tested
Inhibition of recombinant human APE1 using 5'-F-GCCCCCXGGGGACGTACGATATCCCGCTCC-3' as substrate preincubated for 10 mins followed by substrate addition measured at 5 mins intervals for 30 mins by fluorescence-based assay
Assay data:3 Active, 3 Tested
Inhibition of APE1 (unknown origin)
Inhibition of human APE1 preincubated for 15 mins followed by substrate addition by HTS assay
Assay data:8 Active, 7 Activity ≤ 1 µM, 8 Tested
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