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Target
Tyrosyl-DNA phosphodiesterase 2 [E242G,S244A,Q278R,I281T,K282R,R316G,P318T,Y321CH323L]
Ligand
BDBM188529
Substrate
n/a
Meas. Tech.
Recombinant TDP2 Assay
pH
7.5±n/a
IC50
29± 10 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 [E242G,S244A,Q278R,I281T,K282R,R316G,P318T,Y321CH323L]
Synonyms:
TYDP2_MOUSE | Tdp2 | Ttrap | Tyrosyl-DNA phosphodiesterase 2 mutant 9M(mTDP2 9M)
Type:
Protein
Mol. Mass.:
40804.32
Organism:
Mus musculus (Mouse)
Description:
The mTDP2 9M bears the mutations at residues Q278R, I281T, K282R, P318T, Y321C, E242G, S244A, R316G, and H323L.
Residue:
370
Sequence:
MASGSSSDAAEPAGPAGRAASAPEAAQAEEDRVKRRRLQCLGFALVGGCDPTMVPSVLRENDWQTQKALSAYFELPENDQGWPRQPPTSFKSEAYVDLTNEDANDTTILEASPSGTPLEDSSTISFITWNIDGLDGCNLPERARGVCSCLALYSPDVVFLQEVIPPYCAYLKKRAASYTIITGNEEGYFTAILLKKGRVKFKSQEIIPFPNTKMMRNLLCVNVSLGGNEFCLMTSHLESTRGHAAERIRQLKTVLGKMQEAPDSTTVIFAGDTNLRDREVTRCGGLPDNVFDAWEFLGKPKHCQYTWDTKANNNLGITAACKLRFDRIFFRAEEGHLIPQSLDLVGLEKLDCGRFPSDHWGLLCTLNVVL
  
Inhibitor
Name:
BDBM188529
Synonyms:
2,4-Dioxo-10-[3-(1H-tetrazol-5-yl)phenyl]pyrimido[4,5-b]-quinoline-8-carbonitrile (1)
Type:
Small organic molecule
Emp. Form.:
C19H10N8O2
Mol. Mass.:
382.3351
SMILES:
O=c1nc2n(-c3cccc(c3)-n3cnnn3)c3cc(ccc3cc2c(=O)[nH]1)C#N
Structure:
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