Ki Summary

Reaction Details

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Target

Tyrosyl-DNA phosphodiesterase 2 [E242G,S244A,Q278R,I281T,K282R,R316G,P318T,Y321CH323L]

Ligand

BDBM188529

Substrate/Competitor

n/a

Meas. Tech.

Recombinant TDP2 Assay

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 Biol11:1925-33 (2016) [PubMed] Article

More Info.:

Get all data from this article, Assay Method

Tyrosyl-DNA phosphodiesterase 2 [E242G,S244A,Q278R,I281T,K282R,R316G,P318T,Y321CH323L]

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:

MASGSSSDAAEPAGPAGRAASAPEAAQAEEDRVKRRRLQCLGFALVGGCDPTMVPSVLRE
NDWQTQKALSAYFELPENDQGWPRQPPTSFKSEAYVDLTNEDANDTTILEASPSGTPLED
SSTISFITWNIDGLDGCNLPERARGVCSCLALYSPDVVFLQEVIPPYCAYLKKRAASYTI
ITGNEEGYFTAILLKKGRVKFKSQEIIPFPNTKMMRNLLCVNVSLGGNEFCLMTSHLEST
RGHAAERIRQLKTVLGKMQEAPDSTTVIFAGDTNLRDREVTRCGGLPDNVFDAWEFLGKP
KHCQYTWDTKANNNLGITAACKLRFDRIFFRAEEGHLIPQSLDLVGLEKLDCGRFPSDHW
GLLCTLNVVL

BDBM188529

n/a

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