Reaction Details |
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Target | Protein mono-ADP-ribosyltransferase PARP10 |
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Ligand | BDBM27566 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1646312 (CHEMBL3995368) |
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IC50 | 1259±n/a nM |
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Citation | Thorsell, AG; Ekblad, T; Karlberg, T; Löw, M; Pinto, AF; Trésaugues, L; Moche, M; Cohen, MS; Schüler, H Structural Basis for Potency and Promiscuity in Poly(ADP-ribose) Polymerase (PARP) and Tankyrase Inhibitors. J Med Chem60:1262-1271 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Protein mono-ADP-ribosyltransferase PARP10 |
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Name: | Protein mono-ADP-ribosyltransferase PARP10 |
Synonyms: | 2.4.2.- | 2.4.2.30 | ADP-ribosyltransferase diphtheria toxin-like 10 | ARTD10 | Human diphtheria toxin-like ADP-ribosyltransferase (ARTD10 or PARP10, L926Y)) | Human diphtheria toxin-like ADP-ribosyltransferase (ARTD10 or PARP10, R931A)) | Human diphtheria toxin-like ADP-ribosyltransferase (ARTD10 or PARP10, S927A)) | PAR10_HUMAN | PARP-10 | PARP10 | Poly [ADP-ribose] polymerase 10 |
Type: | n/a |
Mol. Mass.: | 109953.63 |
Organism: | Homo sapiens (Human) |
Description: | Q53GL7 |
Residue: | 1025 |
Sequence: | MVAMAEAEAGVAVEVRGLPPAVPDELLTLYFENRRRSGGGPVLSWQRLGCGGVLTFREPA
DAERVLAQADHELHGAQLSLRPAPPRAPARLLLQGLPPGTTPQRLEQHVQALLRASGLPV
QPCCALASPRPDRALVQLPKPLSEADVRVLEEQAQNLGLEGTLVSLARVPQARAVRVVGD
GASVDLLLLELYLENERRSGGGPLEDLQRLPGPLGTVASFQQWQVAERVLQQEHRLQGSE
LSLVPHYDILEPEELAENTSGGDHPSTQGPRATKHALLRTGGLVTALQGAGTVTMGSGEE
PGQSGASLRTGPMVQGRGIMTTGSGQEPGQSGTSLRTGPMGSLGQAEQVSSMPMGSLEHE
GLVSLRPVGLQEQEGPMSLGPVGSAGPVETSKGLLGQEGLVEIAMDSPEQEGLVGPMEIT
MGSLEKAGPVSPGCVKLAGQEGLVEMVLLMEPGAMRFLQLYHEDLLAGLGDVALLPLEGP
DMTGFRLCGAQASCQAAEEFLRSLLGSISCHVLCLEHPGSARFLLGPEGQHLLQGLEAQF
QCVFGTERLATATLDTGLEEVDPTEALPVLPGNAHTLWTPDSTGGDQEDVSLEEVRELLA
TLEGLDLDGEDWLPRELEEEGPQEQPEEEVTPGHEEEEPVAPSTVAPRWLEEEAALQLAL
HRSLEPQGQVAEQEEAAALRQALTLSLLEQPPLEAEEPPDGGTDGKAQLVVHSAFEQDVE
ELDRALRAALEVHVQEETVGPWRRTLPAELRARLERCHGVSVALRGDCTILRGFGAHPAR
AARHLVALLAGPWDQSLAFPLAASGPTLAGQTLKGPWNNLERLAENTGEFQEVVRAFYDT
LDAARSSIRVVRVERVSHPLLQQQYELYRERLLQRCERRPVEQVLYHGTTAPAVPDICAH
GFNRSFCGRNATVYGKGVYFARRASLSVQDRYSPPNADGHKAVFVARVLTGDYGQGRRGL
RAPPLRGPGHVLLRYDSAVDCICQPSIFVIFHDTQALPTHLITCEHVPRASPDDPSGLPG
RSPDT
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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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