Reaction Details |
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Target | Protein mono-ADP-ribosyltransferase PARP10 |
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Ligand | BDBM50272952 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1712748 (CHEMBL4122797) |
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IC50 | 513±n/a nM |
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Citation | Holechek, J; Lease, R; Thorsell, AG; Karlberg, T; McCadden, C; Grant, R; Keen, A; Callahan, E; Schüler, H; Ferraris, D Design, synthesis and evaluation of potent and selective inhibitors of mono-(ADP-ribosyl)transferases PARP10 and PARP14. Bioorg Med Chem Lett28:2050-2054 (2018) [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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BDBM50272952 |
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n/a |
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Name | BDBM50272952 |
Synonyms: | CHEMBL4126054 |
Type | Small organic molecule |
Emp. Form. | C14H12N2O3 |
Mol. Mass. | 256.2567 |
SMILES | NC(=O)c1ccc(Oc2cccc(c2)C(N)=O)cc1 |
Structure |
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