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Target
Tyrosyl-DNA phosphodiesterase 2
Ligand
BDBM50521702
Substrate
n/a
Meas. Tech.
ChEMBL_1884986 (CHEMBL4386568)
IC50
130±n/a nM
Citation
 Kankanala, J; Ribeiro, CJA; Kiselev, E; Ravji, A; Williams, J; Xie, J; Aihara, H; Pommier, Y; Wang, Z Novel Deazaflavin Analogues Potently Inhibited Tyrosyl DNA Phosphodiesterase 2 (TDP2) and Strongly Sensitized Cancer Cells toward Treatment with Topoisomerase II (TOP2) Poison Etoposide. J Med Chem 62:4669-4682 (2019) [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:
BDBM50521702
Synonyms:
CHEMBL4518508
Type:
Small organic molecule
Emp. Form.:
C26H16N4O5
Mol. Mass.:
464.429
SMILES:
OC(=O)c1cccc(COc2ccc(cc2)-n2c3cc(ccc3cc3c2nc(=O)[nH]c3=O)C#N)c1
Structure:
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