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Target
Tyrosyl-DNA phosphodiesterase 2
Ligand
BDBM50374211
Substrate
n/a
Meas. Tech.
ChEMBL_1737948 (CHEMBL4153698)
IC50
17000±n/a nM
Citation
 Yu, LM; Hu, Z; Chen, Y; Ravji, A; Lopez, S; Plescia, CB; Yu, Q; Yang, H; Abdelmalak, M; Saha, S; Agama, K; Kiselev, E; Marchand, C; Pommier, Y; An, LK Synthesis and structure-activity relationship of furoquinolinediones as inhibitors of Tyrosyl-DNA phosphodiesterase 2 (TDP2). Eur J Med Chem 151:777-796 (2018) [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:
BDBM50374211
Synonyms:
CHEMBL4173396
Type:
Small organic molecule
Emp. Form.:
C25H20N2O8
Mol. Mass.:
476.4349
SMILES:
COC(=O)[C@H](Cc1ccc(OC(=O)c2c(C)oc3c2C(=O)c2ncccc2C3=O)cc1)NC(C)=O |r|
Structure:
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