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Target
Protein mono-ADP-ribosyltransferase PARP6
Ligand
BDBM27566
Substrate
n/a
Meas. Tech.
ChEMBL_1541482 (CHEMBL3743853)
IC50
1800±n/a nM
Citation
 Johannes, JW; Almeida, L; Daly, K; Ferguson, AD; Grosskurth, SE; Guan, H; Howard, T; Ioannidis, S; Kazmirski, S; Lamb, ML; Larsen, NA; Lyne, PD; Mikule, K; Ogoe, C; Peng, B; Petteruti, P; Read, JA; Su, N; Sylvester, M; Throner, S; Wang, W; Wang, X; Wu, J; Ye, Q; Yu, Y; Zheng, X; Scott, DA Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering. Bioorg Med Chem Lett 25:5743-7 (2015) [PubMed]  Article 
Target
Name:
Protein mono-ADP-ribosyltransferase PARP6
Synonyms:
ADP-ribosyltransferase diphtheria toxin-like 17 | ARTD17 | PARP-6 | PARP6 | PARP6_HUMAN | Poly [ADP-ribose] polymerase 6
Type:
PROTEIN
Mol. Mass.:
71130.07
Organism:
Homo sapiens (Human)
Description:
ChEMBL_107589
Residue:
630
Sequence:
MDIKGQFWNDDDSEGDNESEEFLYGVQGSCAADLYRHPQLDADIEAVKEIYSENSVSIREYGTIDDVDIDLHINISFLDEEVSTAWKVLRTEPIVLRLRFSLSQYLDGPEPSIEVFQPSNKEGFGLGLQLKKILGMFTSQQWKHLSNDFLKTQQEKRHSWFKASGTIKKFRAGLSIFSPIPKSPSFPIIQDSMLKGKLGVPELRVGRLMNRSISCTMKNPKVEVFGYPPSPQAGLLCPQHVGLPPPARTSPLVSGHCKNIPTLEYGFLVQIMKYAEQRIPTLNEYCVVCDEQHVFQNGSMLKPAVCTRELCVFSFYTLGVMSGAAEEVATGAEVVDLLVAMCRAALESPRKSIIFEPYPSVVDPTDPKTLAFNPKKKNYERLQKALDSVMSIREMTQGSYLEIKKQMDKLDPLAHPLLQWIISSNRSHIVKLPLSRLKFMHTSHQFLLLSSPPAKEARFRTAKKLYGSTFAFHGSHIENWHSILRNGLVNASYTKLQLHGAAYGKGIYLSPISSISFGYSGMGKGQHRMPSKDELVQRYNRMNTIPQTRSIQSRFLQSRNLNCIALCEVITSKDLQKHGNIWVCPVSDHVCTRFFFVYEDGQVGDANINTQDPKIQKEIMRVIGTQVYTN
  
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
Structure:
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