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TargetHuman diphtheria toxin-like ADP-ribosyltransferase (ARTD6 or PARP5b)
LigandBDBM191195
Substrate/Competitorn/a
Meas. Tech.Biochemical Assay
Temperature298.15±n/a K
IC50 2.5±0.7 nM
Commentsextracted
Citation Cheung, AKChin, DNFan, JMiller-Moslin, KMShultz, MDSmith, TDTomlinson, RCToure, BVisser, MSChen, Z 2-piperidin-1-yl-acetamide compounds for use as tankyrase inhibitors US Patent US9181266 Publication Date 11/10/2015
More Info.:Get all data from this article,  Assay Method
 
Human diphtheria toxin-like ADP-ribosyltransferase (ARTD6 or PARP5b)
Name:Tankyrase 1/2
Synonyms:(ARTD6 or PARP5b) | Tankyrase 1/2 | Tankyrase-1 (TNKS1) | Tankyrase-2 | Tankyrase-2 (TNKS-2) | Tankyrase-2 (TNKS2)
Type:Enzyme
Mol. Mass.:126937.16
Organism:Homo sapiens (Human)
Description:Q9H2K2
Residue:1166
Sequence:
MSGRRCAGGGAACASAAAEAVEPAARELFEACRNGDVERVKRLVTPEKVNSRDTAGRKST
PLHFAAGFGRKDVVEYLLQNGANVQARDDGGLIPLHNACSFGHAEVVNLLLRHGADPNAR
DNWNYTPLHEAAIKGKIDVCIVLLQHGAEPTIRNTDGRTALDLADPSAKAVLTGEYKKDE
LLESARSGNEEKMMALLTPLNVNCHASDGRKSTPLHLAAGYNRVKIVQLLLQHGADVHAK
DKGDLVPLHNACSYGHYEVTELLVKHGACVNAMDLWQFTPLHEAASKNRVEVCSLLLSYG
ADPTLLNCHNKSAIDLAPTPQLKERLAYEFKGHSLLQAAREADVTRIKKHLSLEMVNFKH
PQTHETALHCAAASPYPKRKQICELLLRKGANINEKTKEFLTPLHVASEKAHNDVVEVVV
KHEAKVNALDNLGQTSLHRAAYCGHLQTCRLLLSYGCDPNIISLQGFTALQMGNENVQQL
LQEGISLGNSEADRQLLEAAKAGDVETVKKLCTVQSVNCRDIEGRQSTPLHFAAGYNRVS
VVEYLLQHGADVHAKDKGGLVPLHNACSYGHYEVAELLVKHGAVVNVADLWKFTPLHEAA
AKGKYEICKLLLQHGADPTKKNRDGNTPLDLVKDGDTDIQDLLRGDAALLDAAKKGCLAR
VKKLSSPDNVNCRDTQGRHSTPLHLAAGYNNLEVAEYLLQHGADVNAQDKGGLIPLHNAA
SYGHVDVAALLIKYNACVNATDKWAFTPLHEAAQKGRTQLCALLLAHGADPTLKNQEGQT
PLDLVSADDVSALLTAAMPPSALPSCYKPQVLNGVRSPGATADALSSGPSSPSSLSAASS
LDNLSGSFSELSSVVSSSGTEGASSLEKKEVPGVDFSITQFVRNLGLEHLMDIFEREQIT
LDVLVEMGHKELKEIGINAYGHRHKLIKGVERLISGQQGLNPYLTLNTSGSGTILIDLSP
DDKEFQSVEEEMQSTVREHRDGGHAGGIFNRYNILKIQKVCNKKLWERYTHRRKEVSEEN
HNHANERMLFHGSPFVNAIIHKGFDERHAYIGGMFGAGIYFAENSSKSNQYVYGIGGGTG
CPVHKDRSCYICHRQLLFCRVTLGKSFLQFSAMKMAHSPPGHHSVTGRPSVNGLALAEYV
IYRGEQAYPEYLITYQIMRPEGMVDG
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM191195
NameBDBM191195
Synonyms:US9181266, 64
TypeSmall organic molecule
Emp. Form.C26H30F2N4O5
Mol. Mass.516.537
SMILESCOc1ccc2C(=O)C3(Cc2c1)CCN(CC(=O)N(CC(F)F)Cc1nc2CCOCc2c(=O)[nH]1)CC3
Structure
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n/a