| Reaction Details |
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 | Report a problem with these data |
| Target | Histone-lysine N-methyltransferase EHMT1 |
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| Ligand | BDBM50448487 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1294378 (CHEMBL3129163) |
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| IC50 | 600000±n/a nM |
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| Citation |  Valente, S; Liu, Y; Schnekenburger, M; Zwergel, C; Cosconati, S; Gros, C; Tardugno, M; Labella, D; Florean, C; Minden, S; Hashimoto, H; Chang, Y; Zhang, X; Kirsch, G; Novellino, E; Arimondo, PB; Miele, E; Ferretti, E; Gulino, A; Diederich, M; Cheng, X; Mai, 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 |
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| More Info.: | Get all data from this article, Assay Method |
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| Histone-lysine N-methyltransferase EHMT1 |
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| Name: | Histone-lysine N-methyltransferase EHMT1 |
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| 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 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 141443.67 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_1450367 |
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| Residue: | 1298 |
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| Sequence: | MAAADAEAVPARGEPQQDCCVKTELLGEETPMAADEGSAEKQAGEAHMAADGETNGSCEN
SDASSHANAAKHTQDSARVNPQDGTNTLTRIAENGVSERDSEAAKQNHVTADDFVQTSVI
GSNGYILNKPALQAQPLRTTSTLASSLPGHAAKTLPGGAGKGRTPSAFPQTPAAPPATLG
EGSADTEDRKLPAPGADVKVHRARKTMPKSVVGLHAASKDPREVREARDHKEPKEEINKN
ISDFGRQQLLPPFPSLHQSLPQNQCYMATTKSQTACLPFVLAAAVSRKKKRRMGTYSLVP
KKKTKVLKQRTVIEMFKSITHSTVGSKGEKDLGASSLHVNGESLEMDSDEDDSEELEEDD
GHGAEQAAAFPTEDSRTSKESMSEADRAQKMDGESEEEQESVDTGEEEEGGDESDLSSES
SIKKKFLKRKGKTDSPWIKPARKRRRRSRKKPSGALGSESYKSSAGSAEQTAPGDSTGYM
EVSLDSLDLRVKGILSSQAEGLANGPDVLETDGLQEVPLCSCRMETPKSREITTLANNQC
MATESVDHELGRCTNSVVKYELMRPSNKAPLLVLCEDHRGRMVKHQCCPGCGYFCTAGNF
MECQPESSISHRFHKDCASRVNNASYCPHCGEESSKAKEVTIAKADTTSTVTPVPGQEKG
SALEGRADTTTGSAAGPPLSEDDKLQGAASHVPEGFDPTGPAGLGRPTPGLSQGPGKETL
ESALIALDSEKPKKLRFHPKQLYFSARQGELQKVLLMLVDGIDPNFKMEHQNKRSPLHAA
AEAGHVDICHMLVQAGANIDTCSEDQRTPLMEAAENNHLEAVKYLIKAGALVDPKDAEGS
TCLHLAAKKGHYEVVQYLLSNGQMDVNCQDDGGWTPMIWATEYKHVDLVKLLLSKGSDIN
IRDNEENICLHWAAFSGCVDIAEILLAAKCDLHAVNIHGDSPLHIAARENRYDCVVLFLS
RDSDVTLKNKEGETPLQCASLNSQVWSALQMSKALQDSAPDRPSPVERIVSRDIARGYER
IPIPCVNAVDSEPCPSNYKYVSQNCVTSPMNIDRNITHLQYCVCIDDCSSSNCMCGQLSM
RCWYDKDGRLLPEFNMAEPPLIFECNHACSCWRNCRNRVVQNGLRARLQLYRTRDMGWGV
RSLQDIPPGTFVCEYVGELISDSEADVREEDSYLFDLDNKDGEVYCIDARFYGNVSRFIN
HHCEPNLVPVRVFMAHQDLRFPRIAFFSTRLIEAGEQLGFDYGERFWDIKGKLFSCRCGS
PKCRHSSAALAQRQASAAQEAQEDGLPDTSSAAAADPL
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| BDBM50448487 |
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| n/a |
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| Name | BDBM50448487 |
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| Synonyms: | CHEMBL2385821 |
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| Type | Small organic molecule |
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| Emp. Form. | C27H23N7O |
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| Mol. Mass. | 461.5178 |
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| SMILES | Cc1cc(Nc2cccc(NC(=O)c3ccc(Nc4ccnc5ccccc45)cc3)c2)nc(N)n1 |
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| Structure | 
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