Reaction Details |
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Target | N-lysine methyltransferase KMT5A |
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Ligand | BDBM50548177 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2020039 (CHEMBL4673852) |
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IC50 | 804±n/a nM |
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Citation | Butler, KV; Ma, A; Yu, W; Li, F; Tempel, W; Babault, N; Pittella-Silva, F; Shao, J; Wang, J; Luo, M; Vedadi, M; Brown, PJ; Arrowsmith, CH; Jin, J Structure-Based Design of a Covalent Inhibitor of the SET Domain-Containing Protein 8 (SETD8) Lysine Methyltransferase. J Med Chem59:9881-9889 (2016) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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N-lysine methyltransferase KMT5A |
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Name: | N-lysine methyltransferase KMT5A |
Synonyms: | KMT5A | KMT5A_HUMAN | N-lysine methyltransferase SETD8 | PRSET7 | SET domain-containing protein 8 (SetD8) | SET07 | SET8 | SETD8 |
Type: | Enzyme |
Mol. Mass.: | 42919.11 |
Organism: | Homo sapiens (Human) |
Description: | Q9NQR1 |
Residue: | 393 |
Sequence: | MGEGGAAAALVAAAAAAAAAAAAVVAGQRRRRLGRRARCHGPGRAAGGKMSKPCAVEAAA
AAVAATAPGPEMVERRGPGRPRTDGENVFTGQSKIYSYMSPNKCSGMRFPLQEENSVTHH
EVKCQGKPLAGIYRKREEKRNAGNAVRSAMKSEEQKIKDARKGPLVPFPNQKSEAAEPPK
TPPSSCDSTNAAIAKQALKKPIKGKQAPRKKAQGKTQQNRKLTDFYPVRRSSRKSKAELQ
SEERKRIDELIESGKEEGMKIDLIDGKGRGVIATKQFSRGDFVVEYHGDLIEITDAKKRE
ALYAQDPSTGCYMYYFQYLSKTYCVDATRETNRLGRLINHSKCGNCQTKLHDIDGVPHLI
LIASRDIAAGEELLYDYGDRSKASIEAHPWLKH
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BDBM50548177 |
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n/a |
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Name | BDBM50548177 |
Synonyms: | CHEMBL4791952 |
Type | Small organic molecule |
Emp. Form. | C20H27N5O3 |
Mol. Mass. | 385.4601 |
SMILES | COc1cc2nc(nc(NCCCNC(=O)C=C)c2cc1OC)N1CCCC1 |
Structure |
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