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Target
Tyrosyl-DNA phosphodiesterase 2
Ligand
BDBM50372749
Substrate
n/a
Meas. Tech.
ChEMBL_1737947 (CHEMBL4153697)
IC50
8100±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:
BDBM50372749
Synonyms:
CHEMBL4164245
Type:
Small organic molecule
Emp. Form.:
C24H18N4O6
Mol. Mass.:
458.4229
SMILES:
Cc1oc2c(c1C(=O)Oc1cccc(c1)-c1cn(CCCO)nn1)C(=O)c1ncccc1C2=O
Structure:
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