Reaction Details Report a problem with these data
Target
DNA-(apurinic or apyrimidinic site) endonuclease
Ligand
BDBM26614
Substrate
DNA Substrate
Meas. Tech.
High-Throughput Screening and IC50 Determinations
pH
7.5±n/a
Temperature
295.15±n/a K
Comments
84% Inhibition uM.
Citation
 Seiple, LA; Cardellina, JH; Akee, R; Stivers, JT Potent inhibition of human apurinic/apyrimidinic endonuclease 1 by arylstibonic acids. Mol Pharmacol 73:669-77 (2008) [PubMed]  Article 
Target
Name:
DNA-(apurinic or apyrimidinic site) endonuclease
Synonyms:
APE | APE1 | APEX | APEX1 | APEX1_HUMAN | APX | Apurinic-apyrimidinic endonuclease 1 (APE-1) | Apurinic/apyrimidinic endonuclease 1 (APE1) | DNA-(apurinic or apyrimidinic site) lyase | HAP1 | REF1
Type:
Protein
Mol. Mass.:
35560.12
Organism:
Homo sapiens (Human)
Description:
P27695
Residue:
318
Sequence:
MPKRGKKGAVAEDGDELRTEPEAKKSKTAAKKNDKEAAGEGPALYEDPPDQKTSPSGKPATLKICSWNVDGLRAWIKKKGLDWVKEEAPDILCLQETKCSENKLPAELQELPGLSHQYWSAPSDKEGYSGVGLLSRQCPLKVSYGIGDEEHDQEGRVIVAEFDSFVLVTAYVPNAGRGLVRLEYRQRWDEAFRKFLKGLASRKPLVLCGDLNVAHEEIDLRNPKGNKKNAGFTPQERQGFGELLQAVPLADSFRHLYPNTPYAYTFWTYMMNARSKNVGWRLDYFLLSHSLLPALCDSKIRSKALGSDHCPITLYLAL
  
Inhibitor
Name:
BDBM26614
Synonyms:
2-[(4-hydroxy-3-methylphenyl)[(1Z)-3-methyl-4-oxocyclohexa-2,5-dien-1-ylidene]methyl]benzoic acid | Compound 10470
Type:
Small organic molecule
Emp. Form.:
C22H18O4
Mol. Mass.:
346.3759
SMILES:
CC1=C\C(C=CC1=O)=C(\c1ccc(O)c(C)c1)c1ccccc1C(O)=O |c:4,t:1|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
DNA Substrate
Synonyms:
Annealed double-stranded oligonucleotide with an abasic site.
Type:
Fluorescent substrate
Mol. Mass.:
1563.78
Organism:
n/a
Description:
The top strand is 5-FAM-GAG AA(F) ATA GTC GCG-3 containing the tetrahydrofuran synthetic abasic residue (F).
Residue:
18
Sequence:
FAMGAGAAFATAGTCGCG