Target
Protein mono-ADP-ribosyltransferase PARP10
Ligand
BDBM50238419
Substrate
n/a
Meas. Tech.
ChEMBL_1663213 (CHEMBL4012894)
IC50
<5012±n/a nM
Citation
 Thomson, DWWagner, AJBantscheff, MBenson, REDittus, LDuempelfeld, BDrewes, GKrause, JMoore, JTMueller, KPoeckel, DRau, CSalzer, EShewchuk, LHopf, CEmery, JGMuelbaier, M Discovery of a Highly Selective Tankyrase Inhibitor Displaying Growth Inhibition Effects against a Diverse Range of Tumor Derived Cell Lines. J Med Chem 60:5455-5471 (2017) [PubMed]  Article 
Target
Name:
Protein mono-ADP-ribosyltransferase PARP10
Synonyms:
PARP10 | 2.4.2.- | ARTD10 | Human diphtheria toxin-like ADP-ribosyltransferase (ARTD10 or PARP10, L926Y)) | PAR10_HUMAN | 2.4.2.30 | ADP-ribosyltransferase diphtheria toxin-like 10 | PARP-10 | Human diphtheria toxin-like ADP-ribosyltransferase (ARTD10 or PARP10, R931A)) | Human diphtheria toxin-like ADP-ribosyltransferase (ARTD10 or PARP10, S927A)) | Poly [ADP-ribose] polymerase 10
Type:
n/a
Mol. Mass.:
109953.63
Organism:
Human
Description:
Q53GL7
Residue:
1025
Sequence:
MVAMAEAEAGVAVEVRGLPPAVPDELLTLYFENRRRSGGGPVLSWQRLGCGGVLTFREPADAERVLAQADHELHGAQLSLRPAPPRAPARLLLQGLPPGTTPQRLEQHVQALLRASGLPVQPCCALASPRPDRALVQLPKPLSEADVRVLEEQAQNLGLEGTLVSLARVPQARAVRVVGDGASVDLLLLELYLENERRSGGGPLEDLQRLPGPLGTVASFQQWQVAERVLQQEHRLQGSELSLVPHYDILEPEELAENTSGGDHPSTQGPRATKHALLRTGGLVTALQGAGTVTMGSGEEPGQSGASLRTGPMVQGRGIMTTGSGQEPGQSGTSLRTGPMGSLGQAEQVSSMPMGSLEHEGLVSLRPVGLQEQEGPMSLGPVGSAGPVETSKGLLGQEGLVEIAMDSPEQEGLVGPMEITMGSLEKAGPVSPGCVKLAGQEGLVEMVLLMEPGAMRFLQLYHEDLLAGLGDVALLPLEGPDMTGFRLCGAQASCQAAEEFLRSLLGSISCHVLCLEHPGSARFLLGPEGQHLLQGLEAQFQCVFGTERLATATLDTGLEEVDPTEALPVLPGNAHTLWTPDSTGGDQEDVSLEEVRELLATLEGLDLDGEDWLPRELEEEGPQEQPEEEVTPGHEEEEPVAPSTVAPRWLEEEAALQLALHRSLEPQGQVAEQEEAAALRQALTLSLLEQPPLEAEEPPDGGTDGKAQLVVHSAFEQDVEELDRALRAALEVHVQEETVGPWRRTLPAELRARLERCHGVSVALRGDCTILRGFGAHPARAARHLVALLAGPWDQSLAFPLAASGPTLAGQTLKGPWNNLERLAENTGEFQEVVRAFYDTLDAARSSIRVVRVERVSHPLLQQQYELYRERLLQRCERRPVEQVLYHGTTAPAVPDICAHGFNRSFCGRNATVYGKGVYFARRASLSVQDRYSPPNADGHKAVFVARVLTGDYGQGRRGLRAPPLRGPGHVLLRYDSAVDCICQPSIFVIFHDTQALPTHLITCEHVPRASPDDPSGLPGRSPDT
  
Inhibitor
Name:
BDBM50238419
Synonyms:
CHEMBL4060134
Type:
Small organic molecule
Emp. Form.:
C24H22N10O2
Mol. Mass.:
482.19
SMILES:
Cn1cnc(c1)C(=O)N1CCN(CC1)C(=O)c1ccc(Nc2nc3ccccc3n3nnnc23)cc1
Structure:
Search PDB for entries with ligand similarity: