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TargetHistone-lysine N-methyltransferase EHMT1
LigandBDBM50300034
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1705438 (CHEMBL4056671)
IC50 11±n/a nM
Citation Xiong, YLi, FBabault, NWu, HDong, AZeng, HChen, XArrowsmith, CHBrown, PJLiu, JVedadi, MJin, J Structure-activity relationship studies of G9a-like protein (GLP) inhibitors. Bioorg Med Chem25:4414-4423 (2017) [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:
BDBM50300034
n/a
NameBDBM50300034
Synonyms:6,7-Dimethoxy-N2,N2-dimethyl-N4-(1-methylpiperidin-4-yl)-quinazoline-2,4-diamine | 6,7-dimethoxy-N2,N2-dimethyl-N4-(1-methylpiperidin-4-yl)quinazoline-2,4-diamine | CHEMBL576260
TypeSmall organic molecule
Emp. Form.C18H27N5O2
Mol. Mass.345.4393
SMILESCOc1cc2nc(nc(NC3CCN(C)CC3)c2cc1OC)N(C)C
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: