Reaction Details |
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Target | Histone-lysine N-methyltransferase EZH2 |
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Ligand | BDBM50205640 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1628509 |
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IC50 | 571±n/a nM |
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Citation | Ansari A; Satalkar S; Patil V; Shete AS; Kaur S; Gupta A; Singh S; Raja M; Severance DL; Bernales S; Chakravarty S; Hung DT; Pham SM; Herrera FJ; Rai R Novel 3-methylindoline inhibitors of EZH2: Design, synthesis and SAR. Bioorg Med Chem Lett 27:217-222 (2017) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Histone-lysine N-methyltransferase EZH2 |
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Name: | Histone-lysine N-methyltransferase EZH2 |
Synonyms: | ENX-1 | EZH2 | Enhancer of zeste homolog 2 (EZH2) | KMT6 | Lysine N-methyltransferase 6 |
Type: | Protein |
Mol. Mass.: | 85367.84 |
Organism: | Homo sapiens (Human) |
Description: | Q15910 |
Residue: | 746 |
Sequence: | MGQTGKKSEKGPVCWRKRVKSEYMRLRQLKRFRRADEVKSMFSSNRQKILERTEILNQEW
KQRRIQPVHILTSVSSLRGTRECSVTSDLDFPTQVIPLKTLNAVASVPIMYSWSPLQQNF
MVEDETVLHNIPYMGDEVLDQDGTFIEELIKNYDGKVHGDRECGFINDEIFVELVNALGQ
YNDDDDDDDGDDPEEREEKQKDLEDHRDDKESRPPRKFPSDKIFEAISSMFPDKGTAEEL
KEKYKELTEQQLPGALPPECTPNIDGPNAKSVQREQSLHSFHTLFCRRCFKYDCFLHPFH
ATPNTYKRKNTETALDNKPCGPQCYQHLEGAKEFAAALTAERIKTPPKRPGGRRRGRLPN
NSSRPSTPTINVLESKDTDSDREAGTETGGENNDKEEEEKKDETSSSSEANSRCQTPIKM
KPNIEPPENVEWSGAEASMFRVLIGTYYDNFCAIARLIGTKTCRQVYEFRVKESSIIAPA
PAEDVDTPPRKKKRKHRLWAAHCRKIQLKKDGSSNHVYNYQPCDHPRQPCDSSCPCVIAQ
NFCEKFCQCSSECQNRFPGCRCKAQCNTKQCPCYLAVRECDPDLCLTCGAADHWDSKNVS
CKNCSIQRGSKKHLLLAPSDVAGWGIFIKDPVQKNEFISEYCGEIISQDEADRRGKVYDK
YMCSFLFNLNNDFVVDATRKGNKIRFANHSVNPNCYAKVMMVNGDHRIGIFAKRAIQTGE
ELFFDYRYSQADALKYVGIEREMEIP
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BDBM50205640 |
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n/a |
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Name | BDBM50205640 |
Synonyms: | CHEMBL3901407 |
Type | Small organic molecule |
Emp. Form. | C23H26N4O2 |
Mol. Mass. | 390.4781 |
SMILES | Cc1cc(C)c(CNC(=O)c2cc(cc3N(CCc23)C2CCCC2)C#N)c(=O)[nH]1 |
Structure |
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