Target

Ligand

Substrate

Meas. Tech.

PARP-1 Enzyme Inhibition Assay

pH

8±n/a

Temperature

296.15±n/a K

Citation

 Moree, WJ; Goldman, P; Demaggio, AJ; Christenson, E; Herendeen, D; Eksterowicz, J; Kesicki, EA; McElligott, DL; Beaton, G Identification of ring-fused pyrazolo pyridin-2-ones as novel poly(ADP-ribose)polymerase-1 inhibitors. Bioorg Med Chem Lett 18:5126-9 (2008) [PubMed]  Article Copy BDB DOI

More Info.:

Get all data from this article,   Solution Info,  Assay Method

Name:

Poly [ADP-ribose] polymerase 1

Synonyms:

(ARTD1 or PARP1) | 2.4.2.- | 2.4.2.30 | ADP-ribosyltransferase diphtheria toxin-like 1 | ADPRT | ADPRT 1 | ARTD1 | DNA ADP-ribosyltransferase PARP1 | Human diphtheria toxin-like ADP-ribosyltransferase (ARTD1 or PARP1) | NAD(+) ADP-ribosyltransferase 1 | NT-PARP-1 | PARP-1 | PARP1 | PARP1_HUMAN | PPOL | Poly [ADP-ribose] polymerase (PARP) | Poly [ADP-ribose] polymerase 1 (PARP) | Poly [ADP-ribose] polymerase 1 (PARP-1) | Poly [ADP-ribose] polymerase 1 (PARP1) | Poly [ADP-ribose] polymerase 1, 24-kDa form | Poly [ADP-ribose] polymerase 1, 28-kDa form | Poly [ADP-ribose] polymerase 1, 89-kDa form | Poly [ADP-ribose] polymerase 1, processed C-terminus | Poly [ADP-ribose] polymerase 1, processed N-terminus | Poly [ADP-ribose] polymerase-1 | Poly(ADP-ribose) polymerase 1 (PARP1) | Poly(ADP-ribose) polymerase-1 (ARTD1/PARP1) | Poly[ADP-ribose] synthase 1 | Protein poly-ADP-ribosyltransferase PARP1 | Synonyms=ADPRT

Type:

n/a

Mol. Mass.:

113114.22

Organism:

Homo sapiens (Human)

Description:

P09874

Residue:

1014

Sequence:

MAESSDKLYRVEYAKSGRASCKKCSESIPKDSLRMAIMVQSPMFDGKVPHWYHFSCFWKVGHSIRHPDVEVDGFSELRWDDQQKVKKTAEAGGVTGKGQDGIGSKAEKTLGDFAAEYAKSNRSTCKGCMEKIEKGQVRLSKKMVDPEKPQLGMIDRWYHPGCFVKNREELGFRPEYSASQLKGFSLLATEDKEALKKQLPGVKSEGKRKGDEVDGVDEVAKKKSKKEKDKDSKLEKALKAQNDLIWNIKDELKKVCSTNDLKELLIFNKQQVPSGESAILDRVADGMVFGALLPCEECSGQLVFKSDAYYCTGDVTAWTKCMVKTQTPNRKEWVTPKEFREISYLKKLKVKKQDRIFPPETSASVAATPPPSTASAPAAVNSSASADKPLSNMKILTLGKLSRNKDEVKAMIEKLGGKLTGTANKASLCISTKKEVEKMNKKMEEVKEANIRVVSEDFLQDVSASTKSLQELFLAHILSPWGAEVKAEPVEVVAPRGKSGAALSKKSKGQVKEEGINKSEKRMKLTLKGGAAVDPDSGLEHSAHVLEKGGKVFSATLGLVDIVKGTNSYYKLQLLEDDKENRYWIFRSWGRVGTVIGSNKLEQMPSKEDAIEHFMKLYEEKTGNAWHSKNFTKYPKKFYPLEIDYGQDEEAVKKLTVNPGTKSKLPKPVQDLIKMIFDVESMKKAMVEYEIDLQKMPLGKLSKRQIQAAYSILSEVQQAVSQGSSDSQILDLSNRFYTLIPHDFGMKKPPLLNNADSVQAKVEMLDNLLDIEVAYSLLRGGSDDSSKDPIDVNYEKLKTDIKVVDRDSEEAEIIRKYVKNTHATTHNAYDLEVIDIFKIEREGECQRYKPFKQLHNRRLLWHGSRTTNFAGILSQGLRIAPPEAPVTGYMFGKGIYFADMVSKSANYCHTSQGDPIGLILLGEVALGNMYELKHASHISKLPKGKHSVKGLGKTTPDPSANISLDGVDVPLGTGISSGVNDTSLLYNEYIVYDIAQVNLKYLLKLKFNFKTSLW

Blast this sequence in BindingDB or PDB

  
Blast E-value cutoff:

Name:

BDBM27703

Synonyms:

3-methyl-5-phenyl-4,5,7-triazatricyclo[7.4.0.0^{2,6}]trideca-1(9),2(6),3-trien-8-one | ring-fused pyrazolo pyridin-2-one, 30

Type:

Small organic molecule

Emp. Form.:

C17H17N3O

Mol. Mass.:

279.3364

SMILES:

Cc1nn(-c2ccccc2)c2[nH]c(=O)c3CCCCc3c12

Structure:

Search PDB for entries with ligand similarity:

Similarity to this molecule at least:

Name:

BDBM27683

Synonyms:

[adenylate-32P]-NAD

Type:

radiolabeled substrate

Emp. Form.:

n/a

Mol. Mass.:

n/a

SMILES:

n/a

Structure: