Reaction Details 
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Histone-lysine N-methyltransferase KMT5C
Ligand
BDBM223981
Substrate
n/a
Meas. Tech.
Scintillation Proximity Assay (SPA)
pH
8±0
Temperature
298.15±0 K
IC50
144±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] ArticleMore Info.:
Target
Name:
Histone-lysine N-methyltransferase KMT5C
Synonyms:
Histone-lysine N-methyltransferase SUV420H2 | KMT5C | KMT5C_HUMAN | Lysine N-methyltransferase 5C | Protein lysine methyltransferase SUV4-20H2 (SUV4-20H2) | SUV420H2 | Su(var)4-20 homolog 2 | Suppressor of variegation 4-20 homolog 2 | Suv4-20h2
Type:
Enzyme
Mol. Mass.:
52147.69
Organism:
Homo sapiens (Human)
Description:
Q86Y97
Residue:
462
Sequence:
MGPDRVTARELCENDDLATSLVLDPYLGFRTHKMNVSPVPPLRRQQHLRSALETFLRQRDLEAAYRALTLGGWTARYFQSRGPRQEAALKTHVYRYLRAFLPESGFTILPCTRYSMETNGAKIVSTRAWKKNEKLELLVGCIAELREADEGLLRAGENDFSIMYSTRKRSAQLWLGPAAFINHDCKPNCKFVPADGNAACVKVLRDIEPGDEVTCFYGEGFFGEKNEHCECHTCERKGEGAFRTRPREPALPPRPLDKYQLRETKRRLQQGLDSGSRQGLLGPRACVHPSPLRRDPFCAACQPLRLPACSARPDTSPLWLQWLPQPQPRVRPRKRRRPRPRRAPVLSTHHAARVSLHRWGGCGPHCRLRGEALVALGQPPHARWAPQQDWHWARRYGLPYVVRVDLRRLAPAPPATPAPAGTPGPILIPKQALAFAPFSPPKRLRLVVSHGSIDLDVGGEEL
Inhibitor
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:
