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TargetPoly [ADP-ribose] polymerase 1
LigandBDBM27102
Substrate/CompetitorBDBM27089
Meas. Tech.In Vitro PARP Enzyme Assay
pH8±n/a
Temperature295.15±n/a K
Ki 110±n/a nM
Citation Penning, TDZhu, GDGandhi, VBGong, JThomas, SLubisch, WGrandel, RWernet, WPark, CHFry, EHLiu, XShi, YKlinghofer, VJohnson, EFDonawho, CKFrost, DJBontcheva-Diaz, VBouska, JJOlson, AMMarsh, KCLuo, YRosenberg, SHGiranda, VL Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer. Bioorg Med Chem16:6965-75 (2008) [PubMed]  Article
More Info.:Get all data from this article,  Inhibition_Run data,   Solution Info,  Assay Method
 
Poly [ADP-ribose] polymerase 1
Name:Poly [ADP-ribose] polymerase 1
Synonyms:(ARTD1 or PARP1) | 2.4.2.30 | ADP-ribosyltransferase diphtheria toxin-like 1 | ADPRT | ADPRT 1 | ARTD1 | Human diphtheria toxin-like ADP-ribosyltransferase (ARTD1 or PARP1) | NAD(+) ADP-ribosyltransferase 1 | PARP 1, 2 and 3 | PARP-1 | PARP1 | 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 | Poly(ADP-ribose) polymerase 1 (PARP1) | Poly(ADP-ribose) polymerase-1 (ARTD1/PARP1) | Poly[ADP-ribose] synthase 1
Type:n/a
Mol. Mass.:113114.22
Organism:Homo sapiens (Human)
Description:P09874
Residue:1014
Sequence:
MAESSDKLYRVEYAKSGRASCKKCSESIPKDSLRMAIMVQSPMFDGKVPHWYHFSCFWKV
GHSIRHPDVEVDGFSELRWDDQQKVKKTAEAGGVTGKGQDGIGSKAEKTLGDFAAEYAKS
NRSTCKGCMEKIEKGQVRLSKKMVDPEKPQLGMIDRWYHPGCFVKNREELGFRPEYSASQ
LKGFSLLATEDKEALKKQLPGVKSEGKRKGDEVDGVDEVAKKKSKKEKDKDSKLEKALKA
QNDLIWNIKDELKKVCSTNDLKELLIFNKQQVPSGESAILDRVADGMVFGALLPCEECSG
QLVFKSDAYYCTGDVTAWTKCMVKTQTPNRKEWVTPKEFREISYLKKLKVKKQDRIFPPE
TSASVAATPPPSTASAPAAVNSSASADKPLSNMKILTLGKLSRNKDEVKAMIEKLGGKLT
GTANKASLCISTKKEVEKMNKKMEEVKEANIRVVSEDFLQDVSASTKSLQELFLAHILSP
WGAEVKAEPVEVVAPRGKSGAALSKKSKGQVKEEGINKSEKRMKLTLKGGAAVDPDSGLE
HSAHVLEKGGKVFSATLGLVDIVKGTNSYYKLQLLEDDKENRYWIFRSWGRVGTVIGSNK
LEQMPSKEDAIEHFMKLYEEKTGNAWHSKNFTKYPKKFYPLEIDYGQDEEAVKKLTVNPG
TKSKLPKPVQDLIKMIFDVESMKKAMVEYEIDLQKMPLGKLSKRQIQAAYSILSEVQQAV
SQGSSDSQILDLSNRFYTLIPHDFGMKKPPLLNNADSVQAKVEMLDNLLDIEVAYSLLRG
GSDDSSKDPIDVNYEKLKTDIKVVDRDSEEAEIIRKYVKNTHATTHNAYDLEVIDIFKIE
REGECQRYKPFKQLHNRRLLWHGSRTTNFAGILSQGLRIAPPEAPVTGYMFGKGIYFADM
VSKSANYCHTSQGDPIGLILLGEVALGNMYELKHASHISKLPKGKHSVKGLGKTTPDPSA
NISLDGVDVPLGTGISSGVNDTSLLYNEYIVYDIAQVNLKYLLKLKFNFKTSLW
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BDBM27102
NameBDBM27102
Synonyms:2-[1-(propan-2-yl)azetidin-2-yl]-1H-1,3-benzodiazole-4-carboxamide | cyclic amine-containing benzimidazole carboxamide, 3a
TypeSmall organic molecule
Emp. Form.C14H18N4O
Mol. Mass.258.3189
SMILESCC(C)N1CCC1c1nc2cccc(C(N)=O)c2[nH]1
Structure
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BDBM27089
NameBDBM27089
Synonyms:[3H] Nicotinamide adenine dinucleotide | [3H]NAD+ | biotinylated NAD+
Typeradiolabeled substrate
Emp. Form.C21H28N7O14P2
Mol. Mass.664.4325
SMILESNC(=O)c1ccc[n+](c1)[C@H]1O[C@@H](COP(O)(=O)OP(O)(=O)OC[C@H]2O[C@H]([C@H](O)[C@@H]2O)n2cnc3c(N)ncnc23)[C@H](O)[C@@H]1O
Structure
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