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Target
Tyrosyl-DNA phosphodiesterase 2
Ligand
BDBM50008923
Substrate
n/a
Meas. Tech.
ChEBML_1661955
IC50
>111000±n/a nM
Citation
 Wang, P; Elsayed, MSA; Plescia, CB; Ravji, A; Redon, CE; Kiselev, E; Marchand, C; Zeleznik, O; Agama, K; Pommier, Y; Cushman, M Synthesis and Biological Evaluation of the First Triple Inhibitors of Human Topoisomerase 1, Tyrosyl-DNA Phosphodiesterase 1 (Tdp1), and Tyrosyl-DNA Phosphodiesterase 2 (Tdp2). J Med Chem 60:3275-3288 (2017) [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:
BDBM50008923
Synonyms:
(S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]florene-3,13-dione | (S)-4-ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione | 4-Ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione | 4-Ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione (CPT, Camptothecin) | 4-Ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione (Camptothecin) | 4-Ethyl-4-hydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione (camptothecin or CPT) | 4-ethyl-4-hydroxy-(4S)-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-dione | CHEMBL65 | Camptothecin (CT) | camptothecine | cid_24360
Type:
Small organic molecule
Emp. Form.:
C20H16N2O4
Mol. Mass.:
348.352
SMILES:
CC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4ccccc4cc3Cn1c2=O |r|
Structure:
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