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Target
Poly [ADP-ribose] polymerase tankyrase-2
Ligand
BDBM318029
Substrate
n/a
Meas. Tech.
Biochemical Assay
IC50
24.5±22.6 nM
Citation
 Chedid, M; Eissa, HO; Engler, TA; Furness, KW; Rank, KB; Woods, TA; Wrobleski, AD Pyrido[2,3-d]pyrimidin-4-one compounds as tankyrase inhibitors US Patent  US9624218 Publication Date 4/18/2017 
Target
Name:
Poly [ADP-ribose] polymerase tankyrase-2
Synonyms:
(ARTD6 or PARP5b) | PARP5B | Poly [ADP-ribose] polymerase tankyrase-2 | TANK2 | TNKL | TNKS2 | TNKS2_HUMAN | TPoly [ADP-ribose] polymerase tankyrase-2 | Tankyrase 2 | Tankyrase II | Tankyrase-2 | Tankyrase-2 (TNKS-2) | Tankyrase-2 (TNKS2)
Type:
Enzyme
Mol. Mass.:
126937.16
Organism:
Homo sapiens (Human)
Description:
Q9H2K2
Residue:
1166
Sequence:
MSGRRCAGGGAACASAAAEAVEPAARELFEACRNGDVERVKRLVTPEKVNSRDTAGRKSTPLHFAAGFGRKDVVEYLLQNGANVQARDDGGLIPLHNACSFGHAEVVNLLLRHGADPNARDNWNYTPLHEAAIKGKIDVCIVLLQHGAEPTIRNTDGRTALDLADPSAKAVLTGEYKKDELLESARSGNEEKMMALLTPLNVNCHASDGRKSTPLHLAAGYNRVKIVQLLLQHGADVHAKDKGDLVPLHNACSYGHYEVTELLVKHGACVNAMDLWQFTPLHEAASKNRVEVCSLLLSYGADPTLLNCHNKSAIDLAPTPQLKERLAYEFKGHSLLQAAREADVTRIKKHLSLEMVNFKHPQTHETALHCAAASPYPKRKQICELLLRKGANINEKTKEFLTPLHVASEKAHNDVVEVVVKHEAKVNALDNLGQTSLHRAAYCGHLQTCRLLLSYGCDPNIISLQGFTALQMGNENVQQLLQEGISLGNSEADRQLLEAAKAGDVETVKKLCTVQSVNCRDIEGRQSTPLHFAAGYNRVSVVEYLLQHGADVHAKDKGGLVPLHNACSYGHYEVAELLVKHGAVVNVADLWKFTPLHEAAAKGKYEICKLLLQHGADPTKKNRDGNTPLDLVKDGDTDIQDLLRGDAALLDAAKKGCLARVKKLSSPDNVNCRDTQGRHSTPLHLAAGYNNLEVAEYLLQHGADVNAQDKGGLIPLHNAASYGHVDVAALLIKYNACVNATDKWAFTPLHEAAQKGRTQLCALLLAHGADPTLKNQEGQTPLDLVSADDVSALLTAAMPPSALPSCYKPQVLNGVRSPGATADALSSGPSSPSSLSAASSLDNLSGSFSELSSVVSSSGTEGASSLEKKEVPGVDFSITQFVRNLGLEHLMDIFEREQITLDVLVEMGHKELKEIGINAYGHRHKLIKGVERLISGQQGLNPYLTLNTSGSGTILIDLSPDDKEFQSVEEEMQSTVREHRDGGHAGGIFNRYNILKIQKVCNKKLWERYTHRRKEVSEENHNHANERMLFHGSPFVNAIIHKGFDERHAYIGGMFGAGIYFAENSSKSNQYVYGIGGGTGCPVHKDRSCYICHRQLLFCRVTLGKSFLQFSAMKMAHSPPGHHSVTGRPSVNGLALAEYVIYRGEQAYPEYLITYQIMRPEGMVDG
  
Inhibitor
Name:
BDBM318029
Synonyms:
2-[4-[(2- Fluorophenyl)methyl]piperazin-1- yl]-8-methyl-3,5,6,7- tetrahydropyrido[2,3-d]pyrimidin- 4-one dihydrochloride | US9624218, Example 30
Type:
Small organic molecule
Emp. Form.:
C19H24FN5O
Mol. Mass.:
357.4252
SMILES:
CN1CCCc2c1nc([nH]c2=O)N1CCN(Cc2ccccc2F)CC1
Structure:
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