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TargetHistone-lysine N-methyltransferase EZH2
LigandBDBM574919
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:
BDBM574919
n/a
NameBDBM574919
Synonyms:6-methyl-N-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)-7-((R)-1-(4-(oxetan-3-ylamino)cyclohexyl)ethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide | US11459315, Example 63
TypeSmall organic molecule
Emp. Form.C27H36N6O3S
Mol. Mass.524.678
SMILESCSc1cc(C)[nH]c(=O)c1CNC(=O)c1c(C)n([C@H](C)C2CCC(CC2)NC2COC2)c2ncncc12 |wU:18.19,(2.54,-2.14,;4.03,-2.54,;4.42,-4.02,;5.91,-4.42,;6.31,-5.91,;7.8,-6.31,;5.22,-7,;3.73,-6.6,;2.64,-7.69,;3.33,-5.11,;1.85,-4.71,;1.45,-3.23,;-.04,-2.83,;-1.13,-3.92,;-.51,-1.36,;.39,-.12,;1.93,-.12,;-.51,1.13,;-.04,2.59,;1.47,2.91,;-1.07,3.74,;-2.58,3.42,;-3.61,4.56,;-3.13,6.03,;-1.62,6.35,;-.59,5.2,;-4.16,7.17,;-5.67,6.85,;-6.96,7.69,;-7.8,6.4,;-6.51,5.56,;-1.98,.65,;-3.31,1.42,;-4.65,.65,;-4.65,-.89,;-3.31,-1.66,;-1.98,-.89,)|
Structure
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