Reaction Details |
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Target | N-lysine methyltransferase KMT5A |
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Ligand | BDBM50051128 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1450359 (CHEMBL3378196) |
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IC50 | 34000±n/a nM |
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Citation | Ma, A; Yu, W; Li, F; Bleich, RM; Herold, JM; Butler, KV; Norris, JL; Korboukh, V; Tripathy, A; Janzen, WP; Arrowsmith, CH; Frye, SV; Vedadi, M; Brown, PJ; Jin, J Discovery of a selective, substrate-competitive inhibitor of the lysine methyltransferase SETD8. J Med Chem57:6822-33 (2014) [PubMed] Article |
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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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BDBM50051128 |
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n/a |
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Name | BDBM50051128 |
Synonyms: | CHEMBL3318296 |
Type | Small organic molecule |
Emp. Form. | C26H42N6O2 |
Mol. Mass. | 470.6507 |
SMILES | COc1cc2nc(nc(NCCCCCN3CCN(CC3)C(C)C)c2cc1OC)N1CCCC1 |
Structure |
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