Target
Tyrosyl-DNA phosphodiesterase 2
Ligand
BDBM188529
Substrate
n/a
Meas. Tech.
TDP2 Assays with Whole Cell Extracts
pH
7.5±n/a
IC50
33±n/a 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:
BDBM188529
Synonyms:
2,4-Dioxo-10-[3-(1H-tetrazol-5-yl)phenyl]pyrimido[4,5-b]-quinoline-8-carbonitrile (1)
Type:
Small organic molecule
Emp. Form.:
C19H10N8O2
Mol. Mass.:
382.3351
SMILES:
O=c1nc2n(-c3cccc(c3)-n3cnnn3)c3cc(ccc3cc2c(=O)[nH]1)C#N
Structure:
Search PDB for entries with ligand similarity: