Reaction Details Report a problem with these data
Target
Tyrosyl-DNA phosphodiesterase 2
Ligand
BDBM50438870
Substrate
n/a
Meas. Tech.
Recombinant TDP2 Assay
pH
7.5±n/a
IC50
3.9e+3± 7e+2 nM
Comments
extracted
Citation
 Marchand, C; Abdelmalak, M; Kankanala, J; Huang, SY; Kiselev, E; Fesen, K; Kurahashi, K; Sasanuma, H; Takeda, S; Aihara, H; Wang, Z; Pommier, 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:
BDBM50438870
Synonyms:
8-Chloro-10-(4-hydroxyphenyl)pyrimido[4,5-b]quinoline-2,4-dione (4) | CHEMBL2420501
Type:
Small organic molecule
Emp. Form.:
C17H10ClN3O3
Mol. Mass.:
339.733
SMILES:
Oc1ccc(cc1)-n1c2cc(Cl)ccc2cc2c1nc(=O)[nH]c2=O
Structure:
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