Reaction Details |
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Target | Histone-lysine N-methyltransferase EHMT1 |
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Ligand | BDBM50268866 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1705438 (CHEMBL4056671) |
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IC50 | 46±n/a nM |
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Citation | Xiong, Y; Li, F; Babault, N; Wu, H; Dong, A; Zeng, H; Chen, X; Arrowsmith, CH; Brown, PJ; Liu, J; Vedadi, M; Jin, J Structure-activity relationship studies of G9a-like protein (GLP) inhibitors. Bioorg Med Chem25:4414-4423 (2017) [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 |
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
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BDBM50268866 |
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n/a |
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Name | BDBM50268866 |
Synonyms: | CHEMBL4090654 |
Type | Small organic molecule |
Emp. Form. | C24H31N5O2 |
Mol. Mass. | 421.5352 |
SMILES | COc1cc2nc(nc(NC3CCN(C)CC3)c2cc1OC)N(C)Cc1ccccc1 |
Structure |
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