Reaction Details |
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Target | Protein mono-ADP-ribosyltransferase PARP6 |
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Ligand | BDBM27566 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1541482 (CHEMBL3743853) |
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IC50 | 1800±n/a nM |
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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 Lett25:5743-7 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Protein mono-ADP-ribosyltransferase PARP6 |
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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: | MDIKGQFWNDDDSEGDNESEEFLYGVQGSCAADLYRHPQLDADIEAVKEIYSENSVSIRE
YGTIDDVDIDLHINISFLDEEVSTAWKVLRTEPIVLRLRFSLSQYLDGPEPSIEVFQPSN
KEGFGLGLQLKKILGMFTSQQWKHLSNDFLKTQQEKRHSWFKASGTIKKFRAGLSIFSPI
PKSPSFPIIQDSMLKGKLGVPELRVGRLMNRSISCTMKNPKVEVFGYPPSPQAGLLCPQH
VGLPPPARTSPLVSGHCKNIPTLEYGFLVQIMKYAEQRIPTLNEYCVVCDEQHVFQNGSM
LKPAVCTRELCVFSFYTLGVMSGAAEEVATGAEVVDLLVAMCRAALESPRKSIIFEPYPS
VVDPTDPKTLAFNPKKKNYERLQKALDSVMSIREMTQGSYLEIKKQMDKLDPLAHPLLQW
IISSNRSHIVKLPLSRLKFMHTSHQFLLLSSPPAKEARFRTAKKLYGSTFAFHGSHIENW
HSILRNGLVNASYTKLQLHGAAYGKGIYLSPISSISFGYSGMGKGQHRMPSKDELVQRYN
RMNTIPQTRSIQSRFLQSRNLNCIALCEVITSKDLQKHGNIWVCPVSDHVCTRFFFVYED
GQVGDANINTQDPKIQKEIMRVIGTQVYTN
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BDBM27566 |
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n/a |
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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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