Reaction Details |
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Target | Histone-lysine N-methyltransferase SETMAR |
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Ligand | BDBM50400778 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_879134 (CHEMBL2209105) |
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IC50 | >100000±n/a nM |
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Citation | Verma, SK; Tian, X; LaFrance, LV; Duquenne, C; Suarez, DP; Newlander, KA; Romeril, SP; Burgess, JL; Grant, SW; Brackley, JA; Graves, AP; Scherzer, DA; Shu, A; Thompson, C; Ott, HM; Aller, GS; Machutta, CA; Diaz, E; Jiang, Y; Johnson, NW; Knight, SD; Kruger, RG; McCabe, MT; Dhanak, D; Tummino, PJ; Creasy, CL; Miller, WH Identification of Potent, Selective, Cell-Active Inhibitors of the Histone Lysine Methyltransferase EZH2. ACS Med Chem Lett3:1091-1096 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Histone-lysine N-methyltransferase SETMAR |
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Name: | Histone-lysine N-methyltransferase SETMAR |
Synonyms: | Histone-lysine N-methyltransferase | HsMar1 | Mariner transposase Hsmar1 | Metnase | SET domain and mariner transposase fusion gene-containing protein | SETMAR | SETMR_HUMAN |
Type: | PROTEIN |
Mol. Mass.: | 78041.10 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_879134 |
Residue: | 684 |
Sequence: | MFAEAAKTTRPCGMAEFKEKPEAPTEQLDVACGQENLPVGAWPPGAAPAPFQYTPDHVVG
PGADIDPTQITFPGCICVKTPCLPGTCSCLRHGENYDDNSCLRDIGSGGKYAEPVFECNV
LCRCSDHCRNRVVQKGLQFHFQVFKTHKKGWGLRTLEFIPKGRFVCEYAGEVLGFSEVQR
RIHLQTKSDSNYIIAIREHVYNGQVMETFVDPTYIGNIGRFLNHSCEPNLLMIPVRIDSM
VPKLALFAAKDIVPEEELSYDYSGRYLNLTVSEDKERLDHGKLRKPCYCGAKSCTAFLPF
DSSLYCPVEKSNISCGNEKEPSMCGSAPSVFPSCKRLTLETMKMMLDKKQIRAIFLFEFK
MGRKAAETTRNINNAFGPGTANERTVQWWFKKFCKGDESLEDEERSGRPSEVDNDQLRAI
IEADPLTTTREVAEELNVNHSTVVRHLKQIGKVKKLDKWVPHELTENQKNRRFEVSSSLI
LRNHNEPFLDRIVTCDEKWILYDNRRRSAQWLDQEEAPKHFPKPILHPKKVMVTIWWSAA
GLIHYSFLNPGETITSEKYAQEIDEMNQKLQRLQLALVNRKGPILLHDNARPHVAQPTLQ
KLNELGYEVLPHPPYSPDLLPTNYHVFKHLNNFLQGKRFHNQQDAENAFQEFVESQSTDF
YATGINQLISRWQKCVDCNGSYFD
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BDBM50400778 |
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n/a |
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Name | BDBM50400778 |
Synonyms: | CHEMBL2204995 |
Type | Small organic molecule |
Emp. Form. | C31H39N7O2 |
Mol. Mass. | 541.6871 |
SMILES | CCCc1cc(C)[nH]c(=O)c1CNC(=O)c1cc(cc2n(ncc12)C(C)C)-c1ccnc(c1)N1CCN(C)CC1 |
Structure |
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