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TargetHuman diphtheria toxin-like ADP-ribosyltransferase (ARTD6 or PARP5b)
LigandBDBM27566
Substrate/Competitorn/a
Meas. Tech.Enzyme Assay
IC50 5.2±n/a nM
Citation Zhang, AMiao, ZYe, NHuan, XSong, ZChen, CChen, YDing, J Substituted [1,2,4]triazolo[4,3-a]pyrazines as PARP-1 inhibitors US Patent US9255106 Publication Date 2/9/2016
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:
BDBM27566
NameBDBM27566
Synonyms:4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbonyl]-4-fluorophenyl}methyl)-1,2-dihydrophthalazin-1-one | Acylpiperazine analogue, 47 | Olaparib | US10174023, AZD2281 | US9187430, AZD-2281 | US9255106, AZD2281
TypeSmall organic molecule
Emp. Form.C24H23FN4O3
Mol. Mass.434.4628
SMILESFc1ccc(Cc2n[nH]c(=O)c3ccccc23)cc1C(=O)N1CCN(CC1)C(=O)C1CC1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
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