Reaction Details |
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Target | Protein mono-ADP-ribosyltransferase PARP10 |
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Ligand | BDBM27497 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1646311 (CHEMBL3995367) |
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IC50 | 5800±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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BDBM27497 |
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n/a |
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Name | BDBM27497 |
Synonyms: | 2-(dimethylamino)-N-(6-oxo-5,6-dihydrophenanthridin-2-yl)acetamide | 2-Dimethylamino-N-(6-oxo-5,6-dihydro-phenanthridin-2-yl)-acetamide | CHEMBL372303 | N-(6-oxo-5,6-dihydro- phenanthridin-2-yl)-N,N-dimethylacetamide | N~2~,N~2~-DIMETHYL-N~1~-(6-OXO-5,6-DIHYDROPHENANTHRIDIN-2-YL)GLYCINAMIDE | PJ34 |
Type | Small organic molecule |
Emp. Form. | C17H17N3O2 |
Mol. Mass. | 295.3358 |
SMILES | CN(C)CC(=O)Nc1ccc2[nH]c(=O)c3ccccc3c2c1 |
Structure |
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