Reaction Details
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Poly [ADP-ribose] polymerase 2
Ligand
BDBM27497
Substrate
BDBM27089
Meas. Tech.
Scintillation Proximity Assay (SPA)
pH
7.8±n/a
Temperature
295.15±n/a K
IC50
62±8 nM
Citation
Eltze, T; Boer, R; Wagner, T; Weinbrenner, S; McDonald, MC; Thiemermann, C; Bürkle, A; Klein, T Imidazoquinolinone, imidazopyridine, and isoquinolindione derivatives as novel and potent inhibitors of the poly(ADP-ribose) polymerase (PARP): a comparison with standard PARP inhibitors. Mol Pharmacol 74:1587-98 (2008) [PubMed] Article More Info.:
Target
Name:
Poly [ADP-ribose] polymerase 2
Synonyms:
2.4.2.- | 2.4.2.30 | ADP-ribosyltransferase diphtheria toxin-like 2 | ADPRT-2 | ARTD2 | Adprt2 | Adprtl2 | Aspartl2 | DNA ADP-ribosyltransferase PARP2 | NAD(+) ADP-ribosyltransferase 2 | PARP-2 | PARP2_MOUSE | Parp2 | Poly (ADP-ribose) Polymerase-2 (PARP-2) | Poly [ADP-ribose] polymerase 2 (Parp2) | Poly [ADP-ribose] polymerase-2 | Poly[ADP-ribose] synthase 2 | Poly[ADP-ribose] synthetase 2 | Protein poly-ADP-ribosyltransferase PARP2 | mPARP-2 | pADPRT-2 | poly-ADP-ribose polymerase 2 (PARP2)
Type:
n/a
Mol. Mass.:
63409.97
Organism:
Mus musculus (Mouse)
Description:
Alexis Biochemicals, Cat. no. ALX-201-064-C020
Residue:
559
Sequence:
MAPRRQRSGSGRRVLNEAKKVDNGNKATEDDSPPGKKMRTCQRKGPMAGGKDADRTKDNRDSVKTLLLKGKAPVDPECAAKLGKAHVYCEGDDVYDVMLNQTNLQFNNNKYYLIQLLEDDAQRNFSVWMRWGRVGKTGQHSLVTCSGDLNKAKEIFQKKFLDKTKNNWEDRENFEKVPGKYDMLQMDYAASTQDESKTKEEETLKPESQLDLRVQELLKLICNVQTMEEMMIEMKYDTKRAPLGKLTVAQIKAGYQSLKKIEDCIRAGQHGRALVEACNEFYTRIPHDFGLSIPPVIRTEKELSDKVKLLEALGDIEIALKLVKSERQGLEHPLDQHYRNLHCALRPLDHESNEFKVISQYLQSTHAPTHKDYTMTLLDVFEVEKEGEKEAFREDLPNRMLLWHGSRLSNWVGILSHGLRVAPPEAPITGYMFGKGIYFADMSSKSANYCFASRLKNTGLLLLSEVALGQCNELLEANPKAQGLLRGKHSTKGMGKMAPSPAHFITLNGSTVPLGPASDTGILNPEGYTLNYNEFIVYSPNQVRMRYLLKIQFNFLQLW
Inhibitor
Name:
BDBM27497
Synonyms:
2-(dimethylamino)-N-(6-oxo-5,6-dihydrophenanthridin-2-yl)acetamide | 2-Dimethylamino-N-(6-oxo-5,6-dihydro-phenanthridin-2-yl)-acetamide | CHEMBL372303 | N-(6-oxo-5,6-dihydro- phenanthridin-2-yl)-N,N-dimethylacetamide | N~2~,N~2~-DIMETHYL-N~1~-(6-OXO-5,6-DIHYDROPHENANTHRIDIN-2-YL)GLYCINAMIDE | PJ34
Type:
Small organic molecule
Emp. Form.:
C17H17N3O2
Mol. Mass.:
295.3358
SMILES:
CN(C)CC(=O)Nc1ccc2[nH]c(=O)c3ccccc3c2c1
Structure:
Substrate
Name:
BDBM27089
Synonyms:
[3H] Nicotinamide adenine dinucleotide | [3H]NAD+ | biotinylated NAD+
Type:
radiolabeled substrate
Emp. Form.:
C21H28N7O14P2
Mol. Mass.:
664.4325
SMILES:
NC(=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:
