Target
Tyrosyl-DNA phosphodiesterase 2
Ligand
BDBM50438863
Substrate
n/a
Meas. Tech.
Recombinant TDP2 Assay
pH
7.5±n/a
IC50
1.4e+2± 3e+1 nM
Comments
extracted
Citation
 Marchand, CAbdelmalak, MKankanala, JHuang, SYKiselev, EFesen, KKurahashi, KSasanuma, HTakeda, SAihara, HWang, ZPommier, Y Deazaflavin Inhibitors of Tyrosyl-DNA Phosphodiesterase 2 (TDP2) Specific for the Human Enzyme and Active against Cellular TDP2. ACS Chem Biol 11:1925-33 (2016) [PubMed]  Article 
Target
Name:
Tyrosyl-DNA phosphodiesterase 2
Synonyms:
EAP2 | EAPII | ETS1-associated protein 2 | ETS1-associated protein II | TDP2 | TRAF and TNF receptor-associated protein | TTRAP | TYDP2_HUMAN | Tyr-DNA phosphodiesterase 2 | Tyrosyl-DNA phosphodiesterase 2 | Tyrosyl-DNA phosphodiesterase 2 (hTDP2) | Tyrosyl-RNA phosphodiesterase | VPg unlinkase | hTDP2
Type:
Enzyme Catalytic Domain
Mol. Mass.:
40916.54
Organism:
Homo sapiens (Human)
Description:
gi_23510348
Residue:
362
Sequence:
MELGSCLEGGREAAEEEGEPEVKKRRLLCVEFASVASCDAAVAQCFLAENDWEMERALNSYFEPPVEESALERRPETISEPKTYVDLTNEETTDSTTSKISPSEDTQQENGSMFSLITWNIDGLDLNNLSERARGVCSYLALYSPDVIFLQEVIPPYYSYLKKRSSNYEIITGHEEGYFTAIMLKKSRVKLKSQEIIPFPSTKMMRNLLCVHVNVSGNELCLMTSHLESTRGHAAERMNQLKMVLKKMQEAPESATVIFAGDTNLRDREVTRCGGLPNNIVDVWEFLGKPKHCQYTWDTQMNSNLGITAACKLRFDRIFFRAAAEEGHIIPRSLDLLGLEKLDCGRFPSDHWGLLCNLDIIL
  
Inhibitor
Name:
BDBM50438863
Synonyms:
10-(4-Hydroxyphenyl)-2,4-dioxo-pyrimido[4,5-b]quinoline-8-carbonitrile (2) | CHEMBL2420465
Type:
Small organic molecule
Emp. Form.:
C18H10N4O3
Mol. Mass.:
330.297
SMILES:
Oc1ccc(cc1)-n1c2cc(ccc2cc2c1nc(=O)[nH]c2=O)C#N
Structure:
Search PDB for entries with ligand similarity: