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TargetHistone-lysine N-methyltransferase EHMT1
LigandBDBM50051117
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1450367 (CHEMBL3378204)
IC50>100000±n/a nM
Citation Ma, AYu, WLi, FBleich, RMHerold, JMButler, KVNorris, JLKorboukh, VTripathy, AJanzen, WPArrowsmith, CHFrye, SVVedadi, MBrown, PJJin, J Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. J Med Chem57:6822-33 (2014) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Histone-lysine N-methyltransferase EHMT1
Name:Histone-lysine N-methyltransferase EHMT1
Synonyms:EHMT1 | EHMT1_HUMAN | EUHMTASE1 | Eu-HMTase1 | Euchromatic histone-lysine N-methyltransferase 1 | G9a-like protein 1 | GLP | GLP1 | H3-K9-HMTase 5 | Histone H3-K9 methyltransferase 5 | Histone-lysine N-methyltransferase EHMT1/EHMT2 | KIAA1876 | KMT1D | Lysine N-methyltransferase 1D
Type:PROTEIN
Mol. Mass.:141443.67
Organism:Homo sapiens (Human)
Description:ChEMBL_1450367
Residue:1298
Sequence:
MAAADAEAVPARGEPQQDCCVKTELLGEETPMAADEGSAEKQAGEAHMAADGETNGSCEN
SDASSHANAAKHTQDSARVNPQDGTNTLTRIAENGVSERDSEAAKQNHVTADDFVQTSVI
GSNGYILNKPALQAQPLRTTSTLASSLPGHAAKTLPGGAGKGRTPSAFPQTPAAPPATLG
EGSADTEDRKLPAPGADVKVHRARKTMPKSVVGLHAASKDPREVREARDHKEPKEEINKN
ISDFGRQQLLPPFPSLHQSLPQNQCYMATTKSQTACLPFVLAAAVSRKKKRRMGTYSLVP
KKKTKVLKQRTVIEMFKSITHSTVGSKGEKDLGASSLHVNGESLEMDSDEDDSEELEEDD
GHGAEQAAAFPTEDSRTSKESMSEADRAQKMDGESEEEQESVDTGEEEEGGDESDLSSES
SIKKKFLKRKGKTDSPWIKPARKRRRRSRKKPSGALGSESYKSSAGSAEQTAPGDSTGYM
EVSLDSLDLRVKGILSSQAEGLANGPDVLETDGLQEVPLCSCRMETPKSREITTLANNQC
MATESVDHELGRCTNSVVKYELMRPSNKAPLLVLCEDHRGRMVKHQCCPGCGYFCTAGNF
MECQPESSISHRFHKDCASRVNNASYCPHCGEESSKAKEVTIAKADTTSTVTPVPGQEKG
SALEGRADTTTGSAAGPPLSEDDKLQGAASHVPEGFDPTGPAGLGRPTPGLSQGPGKETL
ESALIALDSEKPKKLRFHPKQLYFSARQGELQKVLLMLVDGIDPNFKMEHQNKRSPLHAA
AEAGHVDICHMLVQAGANIDTCSEDQRTPLMEAAENNHLEAVKYLIKAGALVDPKDAEGS
TCLHLAAKKGHYEVVQYLLSNGQMDVNCQDDGGWTPMIWATEYKHVDLVKLLLSKGSDIN
IRDNEENICLHWAAFSGCVDIAEILLAAKCDLHAVNIHGDSPLHIAARENRYDCVVLFLS
RDSDVTLKNKEGETPLQCASLNSQVWSALQMSKALQDSAPDRPSPVERIVSRDIARGYER
IPIPCVNAVDSEPCPSNYKYVSQNCVTSPMNIDRNITHLQYCVCIDDCSSSNCMCGQLSM
RCWYDKDGRLLPEFNMAEPPLIFECNHACSCWRNCRNRVVQNGLRARLQLYRTRDMGWGV
RSLQDIPPGTFVCEYVGELISDSEADVREEDSYLFDLDNKDGEVYCIDARFYGNVSRFIN
HHCEPNLVPVRVFMAHQDLRFPRIAFFSTRLIEAGEQLGFDYGERFWDIKGKLFSCRCGS
PKCRHSSAALAQRQASAAQEAQEDGLPDTSSAAAADPL
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50051117
n/a
NameBDBM50051117
Synonyms:CHEMBL3318285
TypeSmall organic molecule
Emp. Form.C23H35N5O2
Mol. Mass.413.5563
SMILESCOc1cc2nc(nc(NCCCCCN3CCCC3)c2cc1OC)N1CCCC1
Structure
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