Reaction Details |
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Target | N-lysine methyltransferase KMT5A |
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Ligand | BDBM50201571 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1623119 (CHEMBL3865471) |
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IC50 | 330±n/a nM |
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Citation | Judge, RA; Zhu, H; Upadhyay, AK; Bodelle, PM; Hutchins, CW; Torrent, M; Marin, VL; Yu, W; Vedadi, M; Li, F; Brown, PJ; Pappano, WN; Sun, C; Petros, AM Turning a Substrate Peptide into a Potent Inhibitor for the Histone Methyltransferase SETD8. ACS Med Chem Lett7:1102-1106 (2016) [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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BDBM50201571 |
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n/a |
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Name | BDBM50201571 |
Synonyms: | CHEMBL3934996 |
Type | Small organic molecule |
Emp. Form. | C49H90N20O10 |
Mol. Mass. | 1119.3669 |
SMILES | CCCCC(NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)NC(C)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O |r| |
Structure |
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