Target
Tyrosyl-DNA phosphodiesterase 2
Ligand
BDBM50438918
Substrate
n/a
Meas. Tech.
ChEMBL_978867 (CHEMBL2423658)
EC50
870±n/a nM
Citation
 Raoof, ADepledge, PHamilton, NMHamilton, NSHitchin, JRHopkins, GVJordan, AMMaguire, LAMcGonagle, AEMould, DPRushbrooke, MSmall, HFSmith, KMThomson, GJTurlais, FWaddell, IDWaszkowycz, BWatson, AJOgilvie, DJ Toxoflavins and deazaflavins as the first reported selective small molecule inhibitors of tyrosyl-DNA phosphodiesterase II. J Med Chem 56:6352-70 (2013) [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:
BDBM50438918
Synonyms:
CHEMBL2094689 | DNDI1417416 | US9073941, 606
Type:
Small organic molecule
Emp. Form.:
C15H15N5O4
Mol. Mass.:
329.3107
SMILES:
COc1ccc(cc1OC)-c1nn(C)c2nc(=O)n(C)c(=O)c2n1
Structure:
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