Reaction Details |
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Target | Histone-lysine N-methyltransferase EHMT1 |
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Ligand | BDBM50353128 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1899415 (CHEMBL4401530) |
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IC50 | 19±n/a nM |
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Citation | Milite, C; Feoli, A; Horton, JR; Rescigno, D; Cipriano, A; Pisapia, V; Viviano, M; Pepe, G; Amendola, G; Novellino, E; Cosconati, S; Cheng, X; Castellano, S; Sbardella, G Discovery of a Novel Chemotype of Histone Lysine Methyltransferase EHMT1/2 (GLP/G9a) Inhibitors: Rational Design, Synthesis, Biological Evaluation, and Co-crystal Structure. J Med Chem62:2666-2689 (2019) [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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BDBM50353128 |
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n/a |
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Name | BDBM50353128 |
Synonyms: | CHEMBL1231795 |
Type | Small organic molecule |
Emp. Form. | C30H47N5O2 |
Mol. Mass. | 509.7265 |
SMILES | COc1cc2c(NC3CCN(CC3)C(C)C)nc(nc2cc1OCCCN1CCCC1)C1CCCCC1 |
Structure |
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