Reaction Details Report a problem with these data
Target
DNA-(apurinic or apyrimidinic site) endonuclease
Ligand
BDBM26621
Substrate
DNA Substrate
Meas. Tech.
High-Throughput Screening and IC50 Determinations
pH
7.5±n/a
Temperature
295.15±n/a K
Ki
19±6 nM
IC50
4±1 nM
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:
BDBM26621
Synonyms:
4-[dihydroxy(oxo)--stibanyl]-2-nitrobenzoic acid | Compound 13755
Type:
Small organic molecule
Emp. Form.:
C7H6NO7Sb
Mol. Mass.:
337.89
SMILES:
OC(=O)c1ccc(cc1[N+]([O-])=O)[Sb](O)(O)=O
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