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Target
Protein mono-ADP-ribosyltransferase PARP10
Ligand
BDBM199181
Substrate
n/a
Meas. Tech.
ChEMBL_1712756 (CHEMBL4122805)
IC50
329±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:
BDBM199181
Synonyms:
4-[(4-Carbamoylcyclohexyl)oxy]cyclohexane-1-carboxamide (OUL35)
Type:
Small organic molecule
Emp. Form.:
C14H12N2O3
Mol. Mass.:
256.2567
SMILES:
NC(=O)c1ccc(Oc2ccc(cc2)C(N)=O)cc1
Structure:
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