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Target
Protein mono-ADP-ribosyltransferase PARP10
Ligand
BDBM50272957
Substrate
n/a
Meas. Tech.
ChEMBL_1712748 (CHEMBL4122797)
IC50
457±n/a nM
Citation
 Holechek, J; Lease, R; Thorsell, AG; Karlberg, T; McCadden, C; Grant, R; Keen, A; Callahan, E; Schüler, H; Ferraris, D Design, synthesis and evaluation of potent and selective inhibitors of mono-(ADP-ribosyl)transferases PARP10 and PARP14. Bioorg Med Chem Lett 28:2050-2054 (2018) [PubMed]  Article 
Target
Name:
Protein mono-ADP-ribosyltransferase PARP10
Synonyms:
2.4.2.- | 2.4.2.30 | ADP-ribosyltransferase diphtheria toxin-like 10 | ARTD10 | Human diphtheria toxin-like ADP-ribosyltransferase (ARTD10 or PARP10, L926Y)) | Human diphtheria toxin-like ADP-ribosyltransferase (ARTD10 or PARP10, R931A)) | Human diphtheria toxin-like ADP-ribosyltransferase (ARTD10 or PARP10, S927A)) | PAR10_HUMAN | PARP-10 | PARP10 | Poly [ADP-ribose] polymerase 10
Type:
n/a
Mol. Mass.:
109953.63
Organism:
Homo sapiens (Human)
Description:
Q53GL7
Residue:
1025
Sequence:
MVAMAEAEAGVAVEVRGLPPAVPDELLTLYFENRRRSGGGPVLSWQRLGCGGVLTFREPADAERVLAQADHELHGAQLSLRPAPPRAPARLLLQGLPPGTTPQRLEQHVQALLRASGLPVQPCCALASPRPDRALVQLPKPLSEADVRVLEEQAQNLGLEGTLVSLARVPQARAVRVVGDGASVDLLLLELYLENERRSGGGPLEDLQRLPGPLGTVASFQQWQVAERVLQQEHRLQGSELSLVPHYDILEPEELAENTSGGDHPSTQGPRATKHALLRTGGLVTALQGAGTVTMGSGEEPGQSGASLRTGPMVQGRGIMTTGSGQEPGQSGTSLRTGPMGSLGQAEQVSSMPMGSLEHEGLVSLRPVGLQEQEGPMSLGPVGSAGPVETSKGLLGQEGLVEIAMDSPEQEGLVGPMEITMGSLEKAGPVSPGCVKLAGQEGLVEMVLLMEPGAMRFLQLYHEDLLAGLGDVALLPLEGPDMTGFRLCGAQASCQAAEEFLRSLLGSISCHVLCLEHPGSARFLLGPEGQHLLQGLEAQFQCVFGTERLATATLDTGLEEVDPTEALPVLPGNAHTLWTPDSTGGDQEDVSLEEVRELLATLEGLDLDGEDWLPRELEEEGPQEQPEEEVTPGHEEEEPVAPSTVAPRWLEEEAALQLALHRSLEPQGQVAEQEEAAALRQALTLSLLEQPPLEAEEPPDGGTDGKAQLVVHSAFEQDVEELDRALRAALEVHVQEETVGPWRRTLPAELRARLERCHGVSVALRGDCTILRGFGAHPARAARHLVALLAGPWDQSLAFPLAASGPTLAGQTLKGPWNNLERLAENTGEFQEVVRAFYDTLDAARSSIRVVRVERVSHPLLQQQYELYRERLLQRCERRPVEQVLYHGTTAPAVPDICAHGFNRSFCGRNATVYGKGVYFARRASLSVQDRYSPPNADGHKAVFVARVLTGDYGQGRRGLRAPPLRGPGHVLLRYDSAVDCICQPSIFVIFHDTQALPTHLITCEHVPRASPDDPSGLPGRSPDT
  
Inhibitor
Name:
BDBM50272957
Synonyms:
CHEMBL4127497
Type:
Small organic molecule
Emp. Form.:
C24H22FN3O3
Mol. Mass.:
419.4482
SMILES:
NC(=O)c1ccc(Oc2cccc(c2)C(=O)N2CCN(CC2)c2ccccc2F)cc1
Structure:
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