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TargetHistone-lysine N-methyltransferase EZH2
LigandBDBM574859
Substrate/Competitorn/a
Meas. Tech.ZH2 biochemical assay (IC50)
IC50 0.5±n/a nM
Citation Brenneman, JBCôté, AGehling, VSKhanna, ALevell, JRMoine, L Modulators of methyl modifying enzymes, compositions and uses thereof US Patent US11459315 Publication Date 10/4/2022
More Info.:Get all data from this article,  Assay Method
 
Histone-lysine N-methyltransferase EZH2
Name:Histone-lysine N-methyltransferase EZH2
Synonyms:ENX-1 | EZH2 | EZH2_HUMAN | Enhancer of zeste homolog 2 (EZH2) | Histone-lysine N-methyltransferase 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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  Blast E-value cutoff:
BDBM574859
n/a
NameBDBM574859
Synonyms:US11459315, Example 18 (isomer 1)
TypeSmall organic molecule
Emp. Form.C27H35N3O3S
Mol. Mass.481.65
SMILESCOC1CC[C@@H](CC1)[C@@H](C)n1c(C)c(C(=O)NCc2c(SC)cc(C)[nH]c2=O)c2ccccc12 |r,wD:5.8,8.9,(9.28,-3.6,;7.71,-3.86,;6.76,-2.5,;5.29,-2.69,;4.38,-1.48,;4.97,-.06,;6.5,.13,;7.38,-1.12,;4.02,1.19,;4.67,2.61,;2.52,.97,;1.46,2.17,;1.82,3.74,;.11,1.59,;-1.28,2.32,;-1.28,3.82,;-2.6,1.51,;-3.95,2.32,;-5.26,1.55,;-5.29,.02,;-3.94,-.82,;-3.94,-2.36,;-6.5,-.71,;-7.96,.02,;-9.28,-.71,;-7.97,1.51,;-6.65,2.32,;-6.65,3.86,;.25,-.02,;-.73,-1.08,;-.3,-2.58,;1.24,-2.87,;2.19,-1.81,;1.71,-.31,)|
Structure
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