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TargetHistone-lysine N-methyltransferase EHMT1
LigandBDBM50448487
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1294378
IC50 600000±n/a nM
Citation Valente, SLiu, YSchnekenburger, MZwergel, CCosconati, SGros, CTardugno, MLabella, DFlorean, CMinden, SHashimoto, HChang, YZhang, XKirsch, GNovellino, EArimondo, PBMiele, EFerretti, EGulino, ADiederich, MCheng, XMai, A Selective non-nucleoside inhibitors of human DNA methyltransferases active in cancer including in cancer stem cells. J Med Chem57:701-13 (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 | EUHMTASE1 | Eu-HMTase1 | Euchromatic histone-lysine N-methyltransferase 1 | G9a-like protein 1 | GLP | GLP1 | H3-K9-HMTase 5 | Histone H3-K9 methyltransferase 5 | 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:
BDBM50448487
NameBDBM50448487
Synonyms:CHEMBL2385821
TypeSmall organic molecule
Emp. Form.C27H23N7O
Mol. Mass.461.5178
SMILESCc1cc(Nc2cccc(NC(=O)c3ccc(Nc4ccnc5ccccc45)cc3)c2)nc(N)n1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least:
n/a