Reaction Details Report a problem with these data
Target
Poly [ADP-ribose] polymerase 2
Ligand
BDBM27566
Substrate
n/a
Meas. Tech.
ChEMBL_2024727 (CHEMBL4678540)
IC50
0.400000±n/a nM
Citation
Wang, H; Ren, B; Liu, Y; Jiang, B; Guo, Y; Wei, M; Luo, L; Kuang, X; Qiu, M; Lv, L; Xu, H; Qi, R; Yan, H; Xu, D; Wang, Z; Huo, CX; Zhu, Y; Zhao, Y; Wu, Y; Qin, Z; Su, D; Tang, T; Wang, F; Sun, X; Feng, Y; Peng, H; Wang, X; Gao, Y; Liu, Y; Gong, W; Yu, F; Liu, X; Wang, L; Zhou, C Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development. J Med Chem 63:15541-15563 (2020) [PubMed] Article
More Info.:
Target
Name:
Poly [ADP-ribose] polymerase 2
Synonyms:
(ARTD2 or PARP2) | ADPRT2 | ADPRTL2 | PARP2 | PARP2_HUMAN | Poly [ADP-ribose] polymerase 2 (PARP-2) | Poly [ADP-ribose] polymerase 2 (PARP2)
Type:
Enzyme
Mol. Mass.:
66225.70
Organism:
Homo sapiens (Human)
Description:
Q9UGN5
Residue:
583
Sequence:
MAARRRRSTGGGRARALNESKRVNNGNTAPEDSSPAKKTRRCQRQESKKMPVAGGKANKDRTEDKQDGMPGRSWASKRVSESVKALLLKGKAPVDPECTAKVGKAHVYCEGNDVYDVMLNQTNLQFNNNKYYLIQLLEDDAQRNFSVWMRWGRVGKMGQHSLVACSGNLNKAKEIFQKKFLDKTKNNWEDREKFEKVPGKYDMLQMDYATNTQDEEETKKEESLKSPLKPESQLDLRVQELIKLICNVQAMEEMMMEMKYNTKKAPLGKLTVAQIKAGYQSLKKIEDCIRAGQHGRALMEACNEFYTRIPHDFGLRTPPLIRTQKELSEKIQLLEALGDIEIAIKLVKTELQSPEHPLDQHYRNLHCALRPLDHESYEFKVISQYLQSTHAPTHSDYTMTLLDLFEVEKDGEKEAFREDLHNRMLLWHGSRMSNWVGILSHGLRIAPPEAPITGYMFGKGIYFADMSSKSANYCFASRLKNTGLLLLSEVALGQCNELLEANPKAEGLLQGKHSTKGLGKMAPSSAHFVTLNGSTVPLGPASDTGILNPDGYTLNYNEYIVYNPNQVRMRYLLKVQFNFLQLW
Inhibitor
Name:
BDBM27566
Synonyms:
4-({3-[(4-cyclopropanecarbonylpiperazin-1-yl)carbonyl]-4-fluorophenyl}methyl)-1,2-dihydrophthalazin-1-one | Acylpiperazine analogue, 47 | Olaparib | US10174023, AZD2281 | US10597399, Compound AZD2281 | US9187430, AZD-2281 | US9255106, AZD2281
Type:
Small organic molecule
Emp. Form.:
C24H23FN4O3
Mol. Mass.:
434.4628
SMILES:
Fc1ccc(Cc2n[nH]c(=O)c3ccccc23)cc1C(=O)N1CCN(CC1)C(=O)C1CC1