Reaction Details |
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Target | Histone-lysine N-methyltransferase KMT5B |
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Ligand | BDBM223981 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Scintillation Proximity Assay (SPA) |
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pH | 8±0 |
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Temperature | 298.15±0 K |
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IC50 | 25±n/a nM |
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Citation | Bromberg, KD; Mitchell, TR; Upadhyay, AK; Jakob, CG; Jhala, MA; Comess, KM; Lasko, LM; Li, C; Tuzon, CT; Dai, Y; Li, F; Eram, MS; Nuber, A; Soni, NB; Manaves, V; Algire, MA; Sweis, RF; Torrent, M; Schotta, G; Sun, C; Michaelides, MR; Shoemaker, AR; Arrowsmith, CH; Brown, PJ; Santhakumar, V; Martin, A; Rice, JC; Chiang, GG; Vedadi, M; Barsyte-Lovejoy, D; Pappano, WN The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity. Nat Chem Biol13:317-324 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Histone-lysine N-methyltransferase KMT5B |
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Name: | Histone-lysine N-methyltransferase KMT5B |
Synonyms: | Histone-lysine N-methyltransferase SUV420H1 | KMT5B | KMT5B_HUMAN | Lysine N-methyltransferase 5B | Protein lysine methyltransferase SUV4-20H1 (SUV4-20H1) | SUV420H1 | Su(var)4-20 homolog 1 | Suppressor of variegation 4-20 homolog 1 | Suv4-20h1 |
Type: | Enzyme |
Mol. Mass.: | 99219.53 |
Organism: | Homo sapiens (Human) |
Description: | Q4FZB7 |
Residue: | 885 |
Sequence: | MKWLGESKNMVVNGRRNGGKLSNDHQQNQSKLQHTGKDTLKAGKNAVERRSNRCNGNSGF
EGQSRYVPSSGMSAKELCENDDLATSLVLDPYLGFQTHKMNTSAFPSRSSRHFSKSDSFS
HNNPVRFRPIKGRQEELKEVIERFKKDEHLEKAFKCLTSGEWARHYFLNKNKMQEKLFKE
HVFIYLRMFATDSGFEILPCNRYSSEQNGAKIVATKEWKRNDKIELLVGCIAELSEIEEN
MLLRHGENDFSVMYSTRKNCAQLWLGPAAFINHDCRPNCKFVSTGRDTACVKALRDIEPG
EEISCYYGDGFFGENNEFCECYTCERRGTGAFKSRVGLPAPAPVINSKYGLRETDKRLNR
LKKLGDSSKNSDSQSVSSNTDADTTQEKNNATSNRKSSVGVKKNSKSRTLTRQSMSRIPA
SSNSTSSKLTHINNSRVPKKLKKPAKPLLSKIKLRNHCKRLEQKNASRKLEMGNLVLKEP
KVVLYKNLPIKKDKEPEGPAQAAVASGCLTRHAAREHRQNPVRGAHSQGESSPCTYITRR
SVRTRTNLKEASDIKLEPNTLNGYKSSVTEPCPDSGEQLQPAPVLQEEELAHETAQKGEA
KCHKSDTGMSKKKSRQGKLVKQFAKIEESTPVHDSPGKDDAVPDLMGPHSDQGEHSGTVG
VPVSYTDCAPSPVGCSVVTSDSFKTKDSFRTAKSKKKRRITRYDAQLILENNSGIPKLTL
RRRHDSSSKTNDQENDGMNSSKISIKLSKDHDNDNNLYVAKLNNGFNSGSGSSSTKLKIQ
LKRDEENRGSYTEGLHENGVCCSDPLSLLESRMEVDDYSQYEEESTDDSSSSEGDEEEDD
YDDDFEDDFIPLPPAKRLRLIVGKDSIDIDISSRRREDQSLRLNA
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BDBM223981 |
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n/a |
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Name | BDBM223981 |
Synonyms: | 6,7-Dichloro-N-cyclopentyl-4-(pyridin-4-yl)phthalazin-1-amine | A-196 (3) |
Type | Small organic molecule |
Emp. Form. | C18H16Cl2N4 |
Mol. Mass. | 359.252 |
SMILES | Clc1cc2c(NC3CCCC3)nnc(-c3ccncc3)c2cc1Cl |
Structure |
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