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Target
Histone-lysine N-methyltransferase KMT5B
Ligand
BDBM223982
Substrate
n/a
Meas. Tech.
Scintillation Proximity Assay (SPA)
pH
8±0
Temperature
298.15±0 K
IC50
>1.0e+4±n/a nM
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 Biol 13:317-324 (2017) [PubMed]  Article 
Target
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:
MKWLGESKNMVVNGRRNGGKLSNDHQQNQSKLQHTGKDTLKAGKNAVERRSNRCNGNSGFEGQSRYVPSSGMSAKELCENDDLATSLVLDPYLGFQTHKMNTSAFPSRSSRHFSKSDSFSHNNPVRFRPIKGRQEELKEVIERFKKDEHLEKAFKCLTSGEWARHYFLNKNKMQEKLFKEHVFIYLRMFATDSGFEILPCNRYSSEQNGAKIVATKEWKRNDKIELLVGCIAELSEIEENMLLRHGENDFSVMYSTRKNCAQLWLGPAAFINHDCRPNCKFVSTGRDTACVKALRDIEPGEEISCYYGDGFFGENNEFCECYTCERRGTGAFKSRVGLPAPAPVINSKYGLRETDKRLNRLKKLGDSSKNSDSQSVSSNTDADTTQEKNNATSNRKSSVGVKKNSKSRTLTRQSMSRIPASSNSTSSKLTHINNSRVPKKLKKPAKPLLSKIKLRNHCKRLEQKNASRKLEMGNLVLKEPKVVLYKNLPIKKDKEPEGPAQAAVASGCLTRHAAREHRQNPVRGAHSQGESSPCTYITRRSVRTRTNLKEASDIKLEPNTLNGYKSSVTEPCPDSGEQLQPAPVLQEEELAHETAQKGEAKCHKSDTGMSKKKSRQGKLVKQFAKIEESTPVHDSPGKDDAVPDLMGPHSDQGEHSGTVGVPVSYTDCAPSPVGCSVVTSDSFKTKDSFRTAKSKKKRRITRYDAQLILENNSGIPKLTLRRRHDSSSKTNDQENDGMNSSKISIKLSKDHDNDNNLYVAKLNNGFNSGSGSSSTKLKIQLKRDEENRGSYTEGLHENGVCCSDPLSLLESRMEVDDYSQYEEESTDDSSSSEGDEEEDDYDDDFEDDFIPLPPAKRLRLIVGKDSIDIDISSRRREDQSLRLNA
  
Inhibitor
Name:
BDBM223982
Synonyms:
(6,7-Dichloro-4-(cyclopentylamino)phthalazin-1-yl)(4-hydroxypiperidin-1-yl)methanone | A-197 (4)
Type:
Small organic molecule
Emp. Form.:
C19H22Cl2N4O2
Mol. Mass.:
409.31
SMILES:
OC1CCN(CC1)C(=O)c1nnc(NC2CCCC2)c2cc(Cl)c(Cl)cc12
Structure:
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